Ketoconazole is an imidazole anti-fungal agent which inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.
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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
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Accessible (Haz class 3, 4, 5 or 8), International
Ketoconazole, an imidazole anti-fungal agent, has often produced features of androgen deficiency including decreased libido, gynecomastia, impotence, oligospermia, and decreased testosterone levels, in men being treated for chronic mycotic infections[6]. It also inhibits arachidonic acid lipoxygenases and cytochrome P-450 enzymes[7]. Ketoconazole competed with [3H]methyltrienolone (R1881) for androgen binding sites in dispersed, intact cultured human skin fibroblasts[6]. In the serum independent HT29-S-B6 colon cell clone, ketoconazole reduced cell proliferation and [3H]thymidine incorporation in a dose-dependent fashion, with a 50% inhibitory concentration of approximately 2.5 μM. It also inhibited [3H]thymidine incorporation in the hormone-independent breast cancer cells MDA-MB-231 and Evsa-T, with respective 50% inhibitory concentration of approximately 13 and 2 μM. In addition, ketoconazole induced a dose-dependent decrease of the number of cells in S phase within 24 h of treatment (from 17 to 3%) and a corresponding increase of the percentage of cells in Go-G1 (from 64 to 80%)[7]. All strains of the seven Malassezia species were susceptible to ketoconazole at low concentrations. M. furfur, M. sympodialis, M. slooffiae, M. pachydermatis, M. globosa, M. obtusa and M. restricta were most sensitive to it with minimum inhibitory concentrations (MICs) ranging from < or = 0.03 to 0.125 μg/mL[8]. Pretreatment with ketoconazole (25 mg/kg, i.p.) significantly decreased plasma corticosterone and reduced low dose (i.e. 0.125 - 0.25 mg/kg per infusion) cocaine self-administration without affecting food-reinforced responding[9]. Ketoconazole raised the AUC of orally administered digoxin from 63 ± 17 to 411 ± 50 μg•h/l. When given intravenously, digoxin AUC increased from 93 ± 22 to 486 ± 26 μg•h/l with ketoconazole administration[10].
Ketoconazole/酮康唑 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
CHO cells
Function assay
Inhibition of CYP24A1 expressed in CHO cells, IC50=0.52 μM
20655626
CHO cells
Function assay
Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=1.90546 μM
18448342
hamster V79MZh11B1 cells
Function assay
Inhibition of human CYP11B1 expressed in hamster V79MZh11B1 cells, IC50=0.127 μM
18672868
hamster V79MZh11B2 cells
Function assay
Inhibition of human CYP11B2 expressed in hamster V79MZh11B2 cells, IC50=0.067 μM
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