1. Anti-infection
  2. Virus Protease
  3. Bevirimat

Bevirimat  (Synonyms: 贝韦立马; PA-457; MPC-4326; YK FH312)

目录号: HY-N0842 纯度: 99.80%
COA 产品使用指南

Bevirimat (PA-457,MPC-4326,YK FH312) 是 HIV-1 病毒颗粒成熟抑制剂。Bevirimat 特定抑制 Gag 加工中最终限速步骤,防止成熟衣壳蛋白 (CA) 从其前体 (CA-SP1) 中释放出来,从而产生未成熟的非传染性病毒颗粒。Bevirimat可用于 HIV-1 感染研究。

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Bevirimat Chemical Structure

Bevirimat Chemical Structure

CAS No. : 174022-42-5

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bevirimat (PA-457, MPC-4326, YK FH312) is an inhibitor of HIV-1 viral particle maturation.Bevirimat specifically inhibits the final rate-limiting step in Gag processing, preventing the release of the mature capsid protein (CA) from its precursor (CA-SP1), resulting in the production of immature non-infectious viral particles. Bevirimat can be used in HIV-1 infection studies[1][2][3][4].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
H9 EC50
< 0.00035 μM
Compound: 2
Anti-HIV activity against acutely infected H9 lymphocytes. Activity expressed as concentration of compound able to suppress HIV replication by 50%.
Anti-HIV activity against acutely infected H9 lymphocytes. Activity expressed as concentration of compound able to suppress HIV replication by 50%.
[PMID: 9804704]
H9 EC50
0.00035 μM
Compound: 133, DSB, PA-457, MPC-4326
Cytotoxicity against human H9 cells after 4 days by coulter counter
Cytotoxicity against human H9 cells after 4 days by coulter counter
[PMID: 20187635]
H9 IC50
7 μM
Compound: 133, DSB, PA-457, MPC-4326
Antiviral activity against HIV1 infected in human H9 cells after 4 days by p24 antigen ELISA
Antiviral activity against HIV1 infected in human H9 cells after 4 days by p24 antigen ELISA
[PMID: 20187635]
H9 IC50
7 μM
Compound: 2
Antiviral activity against HIV1 3B isolate replication in human H9 cells assessed as decrease in viral p24 level after 4 days
Antiviral activity against HIV1 3B isolate replication in human H9 cells assessed as decrease in viral p24 level after 4 days
[PMID: 11141100]
HeLa EC50
> 1 μM
Compound: DSB
Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
[PMID: 19805571]
HeLa EC50
0.009 μM
Compound: DSB
Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
[PMID: 19805571]
HeLa EC50
0.29 μM
Compound: DSB
Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay
[PMID: 19805571]
MT2 CC50
> 10 μM
Compound: bevirimat
Cytotoxicity against mock-infected human MT2 cells assessed as reduction in cell viability incubated for 48 hrs by cell-titer Glo assay
Cytotoxicity against mock-infected human MT2 cells assessed as reduction in cell viability incubated for 48 hrs by cell-titer Glo assay
[PMID: 25927586]
MT2 EC50
> 10000 nM
Compound: 2; BVM
Antiviral activity against wild type HIV1 NL4-3 habouring Gag protein delta V370 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type HIV1 NL4-3 habouring Gag protein delta V370 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
> 10000 nM
Compound: 1
Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 IC50
> 42.78 μM
Compound: 2
Cytotoxicity against MT2 cells by XTT assay
Cytotoxicity against MT2 cells by XTT assay
[PMID: 17935987]
MT2 EC50
0.0013 μM
Compound: 2, Bevirimat
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral replication treated 1 day after infection measured on after 4 days postinfection by p24 antigen ELISA
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral replication treated 1 day after infection measured on after 4 days postinfection by p24 antigen ELISA
[PMID: 20329730]
MT2 EC50
0.005 nM
Compound: PA-457
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days
[PMID: 20660667]
MT2 EC50
0.01 μM
Compound: 1; BVM
Antiviral activity against wild type HIV1 NLRepRlucP373S infected in human MT2 cells after 4 to 5 days by luciferase report gene based multiple cycle drug susceptibility assay
Antiviral activity against wild type HIV1 NLRepRlucP373S infected in human MT2 cells after 4 to 5 days by luciferase report gene based multiple cycle drug susceptibility assay
[PMID: 26968652]
MT2 IC50
0.01 μM
Compound: bevirimat
Antiviral activity against HIV1 NL4.3-Ren infected in human MT2 cells assessed as inhibition of viral growth measured 48 hrs post infection by luminometry
Antiviral activity against HIV1 NL4.3-Ren infected in human MT2 cells assessed as inhibition of viral growth measured 48 hrs post infection by luminometry
[PMID: 25927586]
MT2 EC50
0.011 μM
Compound: 2
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as p24 antigen level after 4 days by ELISA
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as p24 antigen level after 4 days by ELISA
[PMID: 19388685]
MT2 EC50
0.05 nM
Compound: PA-457
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days
[PMID: 20660667]
MT2 EC50
0.5 nM
Compound: PA-457
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days
[PMID: 20660667]
MT2 EC50
0.553 μM
Compound: 1; BVM
Antiviral activity against HIV1 containing gag V370A mutant infected in human MT2 cells after 4 to 5 days by luciferase report gene based multiple cycle drug susceptibility assay
Antiviral activity against HIV1 containing gag V370A mutant infected in human MT2 cells after 4 to 5 days by luciferase report gene based multiple cycle drug susceptibility assay
[PMID: 26968652]
MT2 EC50
0.974 μM
Compound: 1; BVM
Antiviral activity against wild type HIV1 NLRepRlucP373S infected in human MT2 cells after 4 to 5 days in presence of 15 mg/ml HSA by luciferase report gene based multiple cycle drug susceptibility assay
Antiviral activity against wild type HIV1 NLRepRlucP373S infected in human MT2 cells after 4 to 5 days in presence of 15 mg/ml HSA by luciferase report gene based multiple cycle drug susceptibility assay
[PMID: 26968652]
MT2 EC50
10 nM
Compound: 2; BVM
Antiviral activity against wild type HIV1 NL4-3 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type HIV1 NL4-3 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
10 nM
Compound: 1
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
1114 nM
Compound: 1
Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A/T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
1291 nM
Compound: 1
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein in wild type HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum/40% human serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 CC50
16.8 μM
Compound: 1; BVM
Cytotoxicity against human MT2 cells assessed as cell viability by redox dye assay
Cytotoxicity against human MT2 cells assessed as cell viability by redox dye assay
[PMID: 26968652]
MT2 EC50
1810 nM
Compound: 2; BVM
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein V370M mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein V370M mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
1810 nM
Compound: 1
Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370M mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
34 nM
Compound: BVM
Antiviral activity against Human immunodeficiency virus 1 LAI infected in human MT-2 cells by XTT-assay
Antiviral activity against Human immunodeficiency virus 1 LAI infected in human MT-2 cells by XTT-assay
[PMID: 20308382]
MT2 EC50
40 nM
Compound: 2; BVM
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein T371A mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein T371A mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
40 nM
Compound: 1
Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V371A deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 CC50
40 μM
Compound: 2
Cytotoxicity against human MT2 cells by XTT assay
Cytotoxicity against human MT2 cells by XTT assay
[PMID: 19388685]
MT2 IC50
42.78 μM
Compound: 2, Bevirimat
Cytotoxicity against human MT2 cells by XTT assay
Cytotoxicity against human MT2 cells by XTT assay
[PMID: 20329730]
MT2 EC50
552 nM
Compound: 1
Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V370A mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
553 nM
Compound: 2; BVM
Antiviral activity against wild type HIV1 NL4-3 habouring Gag protein V370A mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type HIV1 NL4-3 habouring Gag protein V370A mutant infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
7 nM
Compound: 1
Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein Q369H mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
74 nM
Compound: 1
Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein V3621 mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
77 nM
Compound: 2; BVM
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein delta T371 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
Antiviral activity against wild type BVM-resistant HIV1 NL4-3 habouring Gag protein delta T371 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay
[PMID: 26988305]
MT2 EC50
77 nM
Compound: 1
Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
Binding affinity to gag polyprotein T371 deletion mutant in HIV1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral maturation after 4 to 5 days in presence of 10% fetal bovine serum by dual-luciferase reporter assay
[PMID: 27326328]
MT2 EC50
974 nM
Compound: 2; BVM
Antiviral activity against wild type HIV1 NL4-3 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay in presence of human serum albumin
Antiviral activity against wild type HIV1 NL4-3 infected in human MT2 cells after 4 to 5 days by dual-luciferase reporter gene assay in presence of human serum albumin
[PMID: 26988305]
MT4 CC50
> 10 μM
Compound: 1
Cytotoxicity against human MT4 cells for 4 days
Cytotoxicity against human MT4 cells for 4 days
[PMID: 23379607]
MT4 CC50
> 17 μM
Compound: 1; DSB
Cytotoxicity against human MT4 cells by cell-titer Glo assay
Cytotoxicity against human MT4 cells by cell-titer Glo assay
[PMID: 26598461]
MT4 CC50
> 2 μM
Compound: 3
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 2 days by CytoTox-Glo cytotoxicity assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 2 days by CytoTox-Glo cytotoxicity assay
[PMID: 33639343]
MT4 EC50
> 4 μM
Compound: BVM
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
[PMID: 22818973]
MT4 EC50
> 4 μM
Compound: BVM
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaT371 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaT371 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI
[PMID: 22818973]
MT4 EC50
> 4 μM
Compound: BVM
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaV370 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 deltaV370 mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELI
[PMID: 22818973]
MT4 CC50
> 4.5 μM
Compound: 2
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 2 days by CytoTox-Glo assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 2 days by CytoTox-Glo assay
[PMID: 27676157]
MT4 IC50
> 5 μM
Compound: 1
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370A mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370A mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
[PMID: 23379607]
MT4 IC50
> 5 μM
Compound: 2
Cytotoxicity against human MT4 cells after 4 days
Cytotoxicity against human MT4 cells after 4 days
[PMID: 20673723]
MT4 IC50
> 6.8 μM
Compound: 1
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V362I mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V362I mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
[PMID: 23379607]
MT4 IC50
> 6.8 μM
Compound: 1
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag T371 deletion mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag T371 deletion mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
[PMID: 23379607]
MT4 IC50
> 6.8 μM
Compound: 1
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370 deletion mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
Antiviral activity against 0.001 MOI bevirimat-resistant Human immunodeficiency virus 1 NL4-3 harboring gag V370 deletion mutant infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
[PMID: 23379607]
MT4 CC50
> 6.84 μM
Compound: 3; DSB
Cytotoxicity against human MT4 cells treated for 3 days measured by Celltiter-glo luminescent assay
Cytotoxicity against human MT4 cells treated for 3 days measured by Celltiter-glo luminescent assay
[PMID: 33214842]
MT4 IC50
0.065 μM
Compound: 2
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by p24 ELISA
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by p24 ELISA
[PMID: 27676157]
MT4 EC50
0.075 μM
Compound: 1; DSB
Antiviral activity against HIV-1 NL4-3 infected in MT4 cells assessed inhibition of viral replication measured on day 4 postinfection by ELISA
Antiviral activity against HIV-1 NL4-3 infected in MT4 cells assessed inhibition of viral replication measured on day 4 postinfection by ELISA
[PMID: 26598461]
MT4 EC50
0.076 μM
Compound: BVM
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
[PMID: 22818973]
MT4 IC50
0.076 μM
Compound: 1
Antiviral activity against 0.001 MOI wild type Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
Antiviral activity against 0.001 MOI wild type Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication measured 4 days post infection by ELISA
[PMID: 23379607]
MT4 IC50
0.087 μM
Compound: 2, Bervirimat, DSB, MPC-4326
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as p24 antigen level after 4 days by ELISA
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as p24 antigen level after 4 days by ELISA
[PMID: 22978745]
MT4 EC50
0.096 μM
Compound: 2
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication after 4 days by p24 antigen based ELISA assay
Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication after 4 days by p24 antigen based ELISA assay
[PMID: 20673723]
MT4 CC50
14.2 μM
Compound: 2, Bervirimat, DSB, MPC-4326
Cytotoxicity against human MT4 cells after 2 days
Cytotoxicity against human MT4 cells after 2 days
[PMID: 22978745]
MT4 IC50
15.2 μM
Compound: PA-457
Cytotoxicity against human MT4 lymphocytes after 48 hrs by MTT assay
Cytotoxicity against human MT4 lymphocytes after 48 hrs by MTT assay
[PMID: 21123066]
MT4 CC50
15.9 μM
Compound: DSB
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescent assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescent assay
[PMID: 30703659]
MT4 IC50
7.71 μM
Compound: 2
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring GagV370A mutant infected in human MT4 cells by p24 ELISA
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring GagV370A mutant infected in human MT4 cells by p24 ELISA
[PMID: 27676157]
THP-1 IC50
54 μM
Compound: 25, bevirimat
Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by AlamarBlue assay
Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by AlamarBlue assay
10.1039/C3MD00282A
体外研究
(In Vitro)

Bevirimat 可抑制野生型 HIV-1 病毒的复制,其平均 IC50 值为 10.3 nM[2]
Bevirimat (72 h) 对感染人 HeLa 细胞的野生型 HIV1 和携带噬菌体 I201V 突变蛋白的 HIV1 具有抗病毒活性,EC50 分别为 0.009 和 0.29 μM[3]
Bevirimat (48 h) 对 mock 感染的人类 MT2 细胞具有细胞毒性,CC50 > 10 μM[4]
Bevirimat (1 day) 对人 MT2 细胞中 HIVIIIB 病毒具有抗病毒活性,EC50 为 0.0013 μM[5]
Bevirimat (48 h) 对人类 MT4 细胞具有细胞毒性,根据 CytoTox-Glo 细胞毒性检测法评估,降低细胞活力,CC50 > 2 μM[6]
Bevirimat (4 days) 对人 MT4 细胞感染的 HIV1NL4-3 病毒具有抗病毒活性 (以 p24 抗原水平评估),IC50 为 0.087 μM[7]
Bevirimat (3 days) 对受 HIV-1 感染的 C8166 细胞具有细胞毒性,平均 CC50 为 53.23 μM[9]
Bevirimat (0-8 μM, 3 days) 对 20% 人血清存在下 C8166 细胞中 HIV-1IIIB 的复制有微弱的抑制作用[9]

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

体内研究
(In Vivo)

Bevirimat (10-100 mg/kg,口服,每天两次,22 天) 能有效抑制 SCID-hu Thy/Liv 小鼠体内 HIV-1 的复制并防止胸腺细胞耗竭[8]

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

Animal Model: Male C.B-17 SCID-hu Thy/Liv mice (implanted with tissues from a single donor; implants were inoculated 18 weeks after implantation with 50 µL of stock virus (500–2,000 50% tissue-culture infectious doses) or RPMI 1640 medium (mock infection) by direct injection)[8]
Dosage: 10, 30, and 100 mg/kg
Administration: Oral gavage (p.o.), beginning 1 day before inoculation by direct injection of the Thy/Liv implants and continuing until implant collection 21 days after inoculation
Result: Inhibited viral replication in a dose-dependent manner, reducing implant HIV-1 RNA by 2.1 log10 copies, p24 by 96%, and Gag-p24+ thymocytes from 7% to <1% at 100 mg/kg per day when compared with untreated mice.
Caused significant protection of the implants from virus-mediated loss of cellularity at 10 and 30 mg/kg per day, from depletion of CD4+CD8+ thymocytes at 100 mg/kg per day, and from a reduction in CD4/CD8 ratio at 30 and 100 mg/kg per day.
Clinical Trial
分子量

584.83

Formula

C36H56O6

CAS 号
性状

固体

颜色

White to off-white

中文名称

贝韦立马

结构分类
初始来源
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 : ≥ 50 mg/mL (85.49 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 1.7099 mL 8.5495 mL 17.0990 mL
5 mM 0.3420 mL 1.7099 mL 3.4198 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)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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 (4.27 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。

    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 (4.27 mM); 悬浊液; 超声加热助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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。
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

g

每只动物的给药体积

μL

动物数量

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: 99.80%

参考文献

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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7099 mL 8.5495 mL 17.0990 mL 42.7475 mL
5 mM 0.3420 mL 1.7099 mL 3.4198 mL 8.5495 mL
10 mM 0.1710 mL 0.8549 mL 1.7099 mL 4.2747 mL
15 mM 0.1140 mL 0.5700 mL 1.1399 mL 2.8498 mL
20 mM 0.0855 mL 0.4275 mL 0.8549 mL 2.1374 mL
25 mM 0.0684 mL 0.3420 mL 0.6840 mL 1.7099 mL
30 mM 0.0570 mL 0.2850 mL 0.5700 mL 1.4249 mL
40 mM 0.0427 mL 0.2137 mL 0.4275 mL 1.0687 mL
50 mM 0.0342 mL 0.1710 mL 0.3420 mL 0.8549 mL
60 mM 0.0285 mL 0.1425 mL 0.2850 mL 0.7125 mL
80 mM 0.0214 mL 0.1069 mL 0.2137 mL 0.5343 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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