2. Anti-infection Metabolic Enzyme/Protease
  3. Fungal Cytochrome P450
  4. (Rac)-Ketoconazole

(Rac)-Ketoconazole  (Synonyms: (Rac)-Ketoconazol; (Rac)-R 41400)

目录号: HY-W422288
产品使用指南

摩尔计算器

(Rac)-Ketoconazole ((Rac)-R 41400) 是一种具有口服活性的抗真菌咪唑类化合物。(Rac)-Ketoconazole 通过抑制真菌细胞膜上的一种关键酶——细胞色素 P450 依赖的 14α-甾醇去甲基化酶 (CYP51)，从而干扰真菌的麦角固醇合成，导致细胞膜的功能障碍，最终抑制真菌的生长和繁殖。(Rac)-Ketoconazole 可用于真菌感染的研究。

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(Rac)-Ketoconazole Chemical Structure

(Rac)-Ketoconazole Chemical Structure

CAS No. : 79156-75-5

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Other Forms of (Rac)-Ketoconazole:

(Rac)-Ketoconazole 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(Rac)-Ketoconazole ((Rac)-R 41400) is an antifungal imidazole compound with oral activity. (Rac)-Ketoconazole interferes with ergosterol synthesis by inhibiting cytochrome P450-dependent 14α-sterol demethylase (CYP51), a key enzyme on the fungal cell membrane, leading to membrane dysfunction and ultimately inhibition of fungal growth and reproduction. (Rac)-Ketoconazole is indicated for studies of fungal infections[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Caco-2 IC50
2.36 μM
Compound: KETOCONAZOLE
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
10.21203/rs.3.rs-23951/v1
Caco-2 CC50
28.62 μM
Compound: KETOCONAZOLE
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
10.21203/rs.3.rs-23951/v1
HEK293 IC50
13 μM
Compound: Ketoconazole
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
[PMID: 21030469]
HEK293 IC50
2.6 μM
Compound: ketoconazole
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
[PMID: 28230985]
HEK293 IC50
27 μM
Compound: Ketoconazole
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
[PMID: 21030469]
HepG2 CC50
51 μM
Compound: ketoconazole
Cytotoxicity against human HepG2 cells by neutral red uptake assay
Cytotoxicity against human HepG2 cells by neutral red uptake assay
[PMID: 17433670]
J774 IC50
< 50 μM
Compound: Ktz
Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay
Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay
[PMID: 19110434]
J774 IC50
< 50 μM
Compound: KTZ
Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay
Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay
[PMID: 18547811]
K562 CC50
102 μM
Compound: 1
Cytotoxicity against human K562 cells after assessed as reduction of cell viability 24 hrs by MTT assay
Cytotoxicity against human K562 cells after assessed as reduction of cell viability 24 hrs by MTT assay
[PMID: 18529046]
LLC-PK1 IC50
3.8 μM
Compound: Ketoconazole
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
4.8 μM
Compound: Ketoconazole
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
6.7 μM
Compound: Ketoconazole
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
THP-1 IC50
44 μM
Compound: KTZ
Cytotoxicity against human THP1 cells after 48 hrs
Cytotoxicity against human THP1 cells after 48 hrs
[PMID: 17960923]
THP-1 IC50
44 μM
Compound: KTZ
Cytotoxicity against human THP1 cells assessed as reduction of cell viability after 48 hrs
Cytotoxicity against human THP1 cells assessed as reduction of cell viability after 48 hrs
[PMID: 17287123]
U-937 CC50
125 μM
Compound: 1
Cytotoxicity against human U937 cells assessed as reduction of cell viability after 24 hrs by MTT assay
Cytotoxicity against human U937 cells assessed as reduction of cell viability after 24 hrs by MTT assay
[PMID: 18529046]
V79 IC50
0.52 μM
Compound: ketoconazole
Inhibition of human recombinant CYP24A1 expressed in chinese hamster V79 cells using [3H-1-beta]calcitriol after 60 mins by scintillation counting
Inhibition of human recombinant CYP24A1 expressed in chinese hamster V79 cells using [3H-1-beta]calcitriol after 60 mins by scintillation counting
[PMID: 20594862]
V79 IC50
127 nM
Compound: KTZ
Inhibition of human CYP11B1 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector
Inhibition of human CYP11B1 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector
[PMID: 24900349]
V79 IC50
67 nM
Compound: KTZ
Inhibition of human CYP11B2 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector
Inhibition of human CYP11B2 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector
[PMID: 24900349]
分子量

531.43

Formula

C26H28Cl2N4O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

(Rac)-Ketoconazole 相关分类

  • 摩尔计算器

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The dilution calculator equation

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)
× = ×
C1   V1   C2   V2
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.

Keywords:

(Rac)-Ketoconazole79156-75-5(Rac)-Ketoconazol (Rac)-R 41400FungalCytochrome P450CYPsAntifungal activitycytochrome P450methylation enzymemembrane functionInhibitorinhibitorinhibit

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