Darunavir (Synonyms: 达芦那韦; TMC114; UIC-94017)

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Darunavir (TMC114) 是一个口服有效的、二代 HIV 蛋白酶抑制剂，对突变型病毒和野生型病毒有类似的抗病毒活性。Darunavir (TMC114) 对实验室 HIV-1 毒株和临床分离株 (IC₅₀ = 0.003；IC₉₀ = 0.009 μM) 有效。细胞毒性小。

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Darunavir Chemical Structure

CAS No. : 206361-99-1

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10 mM * 1 mL in DMSO	￥480	In-stock
5 mg	￥400	In-stock
10 mg	￥600	In-stock
25 mg	￥900	In-stock
50 mg	￥1400	In-stock
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Other Forms of Darunavir:

Darunavir Ethanolate In-stock
Darunavir-d9 询价

MCE 顾客使用本产品发表的 11 篇科研文献

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HIV HIV-1 HIV-2

生物活性
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参考文献

生物活性

Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC₅₀ = 0.003 μM; IC₉₀ = 0.009 μM) with minimal cytotoxicity^[1]^[2].

IC₅₀ & Target

HIV-1

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CCRF-CEM	EC₅₀	10 nM Compound: DRV	Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
CCRF-CEM	EC₅₀	6 nM Compound: DRV	Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
CCRF-CEM	EC₅₀	8 nM Compound: DRV	Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
CCRF-CEM	EC₅₀	9 nM Compound: DRV	Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay	[PMID: 17576848]
HEK293	EC₅₀	0.15 nM Compound: 2, DRV	Antiviral activity against wild type HIV1 clade B isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against wild type HIV1 clade B isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK293	EC₅₀	0.18 nM Compound: 2, DRV	Antiviral activity against wild type HIV1 clade C isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against wild type HIV1 clade C isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK293	EC₅₀	0.23 nM Compound: 2, DRV	Antiviral activity against multidrug resistant HIV1 MDR1 containing protease M46I, I54V, V82A and L90M mutant infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against multidrug resistant HIV1 MDR1 containing protease M46I, I54V, V82A and L90M mutant infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK293	EC₅₀	0.25 nM Compound: 2, DRV	Antiviral activity against wild type HIV1 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against wild type HIV1 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK293	EC₅₀	0.3 nM Compound: 2, DRV	Antiviral activity against wild type HIV1 clade A isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against wild type HIV1 clade A isolated form HIV1 patient infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK293	EC₅₀	0.6 nM Compound: 2, DRV	Antiviral activity against multidrug resistant HIV1 MDRC4 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay Antiviral activity against multidrug resistant HIV1 MDRC4 infected in HEK293 cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter based assay	[PMID: 22708897]
HEK-293T	CC₅₀	> 100 μM Compound: DRV	Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay	[PMID: 35483138]
HEK-293T	CC₅₀	> 100 μM Compound: DRV	Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 33906049]
HEK-293T	CC₅₀	> 100 μM Compound: DRV	Cytotoxicity against human 293T cells measured after 24 hrs by CCK8 assay Cytotoxicity against human 293T cells measured after 24 hrs by CCK8 assay	[PMID: 31734023]
HEK-293T	CC₅₀	> 200 μM Compound: DRV	Cytotoxicity against human HEK-293T cells after 24 hrs by CCK-8 assay Cytotoxicity against human HEK-293T cells after 24 hrs by CCK-8 assay	[PMID: 35278855]
HEK-293T	EC₅₀	13660 nM Compound: darunavir	Antiviral activity against multidrug-resistant HIV1 106-PR infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay Antiviral activity against multidrug-resistant HIV1 106-PR infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay	[PMID: 22148316]
HepG2	CC₅₀	95.5 μM Compound: 2, TMC-114	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay	10.1039/C1MD00147G
MT2	CC₅₀	> 100 μM Compound: DRV	Cytotoxicity against human MT2 cells after 7 days by MTT assay Cytotoxicity against human MT2 cells after 7 days by MTT assay	[PMID: 20439612]
MT2	CC₅₀	> 100 μM Compound: 2, TMC-114	Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay	10.1039/C1MD00147G
MT2	EC₅₀	0.003 μM Compound: DRV	Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay	[PMID: 20439612]
MT2	EC₅₀	0.0039 μM Compound: darunavir, DRV	Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	EC₅₀	0.0068 μM Compound: darunavir, DRV	Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	EC₅₀	0.008 μM Compound: DRV	Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay	[PMID: 20439612]
MT2	EC₅₀	0.008 μM Compound: darunavir, DRV	Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT2	EC₅₀	0.01 μM Compound: DRV	Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay	[PMID: 20439612]
MT2	IC₅₀	1.6 nM Compound: 1, DRV	Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay	[PMID: 19746963]
MT2	EC₅₀	2.3 nM Compound: 2, TMC-114	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay	10.1039/C1MD00147G
MT2	IC₅₀	3 nM Compound: Darunavir	Antiviral activity against HIV-1 LAI infected in MT-2 cells measured after 7 days by MTT assay Antiviral activity against HIV-1 LAI infected in MT-2 cells measured after 7 days by MTT assay	[PMID: 26096678]
MT2	IC₅₀	3 nM Compound: 2, DRV	Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay	[PMID: 23947685]
MT2	CC₅₀	83.1 μM Compound: darunavir, DRV	Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	> 100 nM Compound: DPV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay	[PMID: 18212102]
MT4	EC₅₀	0.0026 μM Compound: DRV	Antiviral activity against HIV1 NL4-3 infected in human MT4 cells by XTT assay Antiviral activity against HIV1 NL4-3 infected in human MT4 cells by XTT assay	[PMID: 26306007]
MT4	EC₅₀	0.003 μM Compound: DRV	Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.003 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.003 μM Compound: darunavir, DRV	Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.0033 μM Compound: darunavir, DRV	Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.0034 μM Compound: darunavir, DRV	Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.0035 μM Compound: DRV	Antiviral activity against wild type HIV1 ERS104P infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay Antiviral activity against wild type HIV1 ERS104P infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay	[PMID: 26107245]
MT4	EC₅₀	0.0058 μM Compound: darunavir, DRV	Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.006 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.009 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.009 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.015 μM Compound: darunavir, DRV	Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.016 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.018 μM Compound: darunavir, DRV	Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.021 μM Compound: darunavir, DRV	Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.025 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.029 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.031 μM Compound: DRV	Antiviral activity against darunavir-resistant HIV1 P10 infected in human MT4 cells by XTT assay Antiviral activity against darunavir-resistant HIV1 P10 infected in human MT4 cells by XTT assay	[PMID: 26306007]
MT4	EC₅₀	0.036 μM Compound: darunavir, DRV	Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.097 μM Compound: DRV	Antiviral activity against darunavir-resistant HIV1 P20 infected in human MT4 cells by XTT assay Antiviral activity against darunavir-resistant HIV1 P20 infected in human MT4 cells by XTT assay	[PMID: 26306007]
MT4	EC₅₀	0.2 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.21 μM Compound: darunavir, DRV	Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	EC₅₀	0.29 μM Compound: DRV	Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay	[PMID: 20439612]
MT4	EC₅₀	0.33 μM Compound: darunavir, DRV	Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay	[PMID: 17371811]
MT4	IC₅₀	10 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M6 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M6 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	EC₅₀	11 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 40% fetal bovine serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 40% fetal bovine serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	11 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay	[PMID: 17620375]
MT4	IC₅₀	11 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M3 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M3 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	EC₅₀	12 nM Compound: DRV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay	[PMID: 19323562]
MT4	EC₅₀	12 nM Compound: DRV	Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 17576848]
MT4	EC₅₀	12 nM Compound: DPV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay	[PMID: 18212102]
MT4	IC₅₀	130 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M10 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M10 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	EC₅₀	15 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay	[PMID: 17620375]
MT4	IC₅₀	16 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M8 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M8 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	EC₅₀	19 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	22 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay	[PMID: 17620375]
MT4	IC₅₀	22 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M5 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M5 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	25 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M9 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M9 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	3 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing wild type protease infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing wild type protease infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	IC₅₀	3.2 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M7 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M7 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	EC₅₀	3.5 μM Compound: DRV	Antiviral activity against darunavir-resistant HIV1 P51 infected in human MT4 cells by XTT assay Antiviral activity against darunavir-resistant HIV1 P51 infected in human MT4 cells by XTT assay	[PMID: 26306007]
MT4	IC₅₀	30 nM Compound: DRV	Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M4 mutant infected in human MT4 cells after 5 days by MTT assay Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M4 mutant infected in human MT4 cells after 5 days by MTT assay	[PMID: 22749283]
MT4	EC₅₀	338 nM Compound: DRV	Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay	[PMID: 19323562]
MT4	EC₅₀	338 nM Compound: DPV	Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas	[PMID: 18212102]
MT4	EC₅₀	4 nM Compound: DRV	Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay	[PMID: 19961222]
MT4	EC₅₀	40 nM Compound: DPV	Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay	[PMID: 18212102]
MT4	EC₅₀	5.6 nM Compound: DRV	Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay	[PMID: 17620375]
MT4	EC₅₀	515 nM Compound: DRV	Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay	[PMID: 19323562]
MT4	EC₅₀	587 nM Compound: DRV	Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay	[PMID: 19323562]
MT4	EC₅₀	587 nM Compound: DPV	Antiviral activity against HIV1 B26 infected in human MT4 cells harboring protease L33F, K45I, M46I, I50V, I54V, A71V, and V82F mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infectio Antiviral activity against HIV1 B26 infected in human MT4 cells harboring protease L33F, K45I, M46I, I50V, I54V, A71V, and V82F mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infectio	[PMID: 18212102]
MT4	EC₅₀	857 nM Compound: DPV	Antiviral activity against HIV1 P25 infected in human MT4 cells harboring protease L10F, G16E, V32I, M46I, I47A, H69Y, I84V, and T91S mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post in Antiviral activity against HIV1 P25 infected in human MT4 cells harboring protease L10F, G16E, V32I, M46I, I47A, H69Y, I84V, and T91S mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post in	[PMID: 18212102]
PBMC	EC₅₀	> 0.025 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-JSL infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-JSL infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.003 μM Compound: DRV	Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.0038 μM Compound: 9; DRV	Antiviral activity against wild type HIV1 ERS104pre infected in human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against wild type HIV1 ERS104pre infected in human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.004 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.0043 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-TM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-TM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.005 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-C infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-C infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.007 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-G infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-G infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.008 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.01 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-MM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-MM infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.011 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.019 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.021 μM Compound: 9; DRV	Antiviral activity against multidrug-resistant HIV1-B infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against multidrug-resistant HIV1-B infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	0.023 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	0.027 μM Compound: DRV	Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay	[PMID: 20439612]
PBMC	EC₅₀	255.2 nM Compound: 9; DRV	Antiviral activity against darunavir-resistant HIV1 20P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against darunavir-resistant HIV1 20P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
PBMC	EC₅₀	43.4 nM Compound: 9; DRV	Antiviral activity against darunavir-resistant HIV1 10P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay Antiviral activity against darunavir-resistant HIV1 10P infected in phytohemagglutinin-activated human PBMC cells assessed as inhibition of virus-induced cytopathic effect measured after 7 days by MTT assay	[PMID: 26799988]
SUP-T1	EC₅₀	0.0025 μM Compound: DRV	Antiviral activity against wild-type HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production pretreated with viral infected SUP-T1 cells for 48 hrs followed by reinfection in TZM-bl cells by Antiviral activity against wild-type HIV1 NL4-3 VSV-G pseudotyped virus infected in human SUP-T1 cells assessed as inhibition of late stage viral production pretreated with viral infected SUP-T1 cells for 48 hrs followed by reinfection in TZM-bl cells by	[PMID: 35483138]
Vero C1008	EC₅₀	> 40 μM Compound: Darunavir	Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days	10.1101/2020.04.03.023846

体外研究
(In Vitro)

Darunavir （TMC114, 1a）具有与其他蛋白酶抑制剂相当的稳定性^[1].
Darunavir （TMC114, UIC-94017）在浓度高达5 μM （IC₅₀s, 0.003 ~ 0.029 μM）的情况下，可阻断暴露于并选择抗Ro 31-8959、MK-639、AG1341或ABT 538的HIV-1_NL4-3变体的感染和复制，但对选择抗VX-478 (IC₅₀, 0.22 μM) 的 HIV-1_NL4-3变体的活性较弱^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

547.66

Formula

C₂₇H₃₇N₃O₇S

CAS 号

206361-99-1

性状

固体

颜色

White to off-white

中文名称

达芦那韦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (182.60 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8260 mL	9.1298 mL	18.2595 mL
5 mM	0.3652 mL	1.8260 mL	3.6519 mL
10 mM	0.1826 mL	0.9130 mL	1.8260 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.56 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.56 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.56 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.91%

选择批次：

Data Sheet (642 KB) SDS (251 KB)

COA (205 KB) HNMR (298 KB) LCMS (90 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Dominique L N G Surleraux, et al. Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. J Med Chem. 2005 Mar 24;48(6):1813-22. [Content Brief]

[2]. Yasuhiro Koh, et al. Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Antimicrob Agents Chemother. 2003 Oct;47(10):3123-9. [Content Brief]

Darunavir 相关分类

Inflammation/Immunology Infection

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8260 mL	9.1298 mL	18.2595 mL	45.6488 mL
	5 mM	0.3652 mL	1.8260 mL	3.6519 mL	9.1298 mL
	10 mM	0.1826 mL	0.9130 mL	1.8260 mL	4.5649 mL
	15 mM	0.1217 mL	0.6087 mL	1.2173 mL	3.0433 mL
	20 mM	0.0913 mL	0.4565 mL	0.9130 mL	2.2824 mL
	25 mM	0.0730 mL	0.3652 mL	0.7304 mL	1.8260 mL
	30 mM	0.0609 mL	0.3043 mL	0.6087 mL	1.5216 mL
	40 mM	0.0456 mL	0.2282 mL	0.4565 mL	1.1412 mL
	50 mM	0.0365 mL	0.1826 mL	0.3652 mL	0.9130 mL
	60 mM	0.0304 mL	0.1522 mL	0.3043 mL	0.7608 mL
	80 mM	0.0228 mL	0.1141 mL	0.2282 mL	0.5706 mL
	100 mM	0.0183 mL	0.0913 mL	0.1826 mL	0.4565 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Darunavir (Synonyms: 达芦那韦; TMC114; UIC-94017)

Customer Review

Other Forms of Darunavir:

MCE 顾客使用本产品发表的 11 篇科研文献

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Darunavir (Synonyms: 达芦那韦; TMC114; UIC-94017)

Customer Review

Other Forms of Darunavir:

Darunavir 相关抗体

MCE 顾客使用本产品发表的 11 篇科研文献

Darunavir 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 HIV 亚型特异性产品:

生物活性

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参考文献

Darunavir 相关抗体:

摩尔计算器

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