Ketoconazole

Ketoconazole is an imidazole anti-fungal agent, a CYP3A4 inhibitor. (In Vitro) :Ketoconazole (R-41400), 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. Ketoconazole (R-41400) also is a cytochrome P450 inhibitor. Ketoconazole (R-41400), on the antischistosomal potential of these quinolines against Schistosoma mansoni infection by evaluating parasitological, histopathological, and biochemical parameters. Mice were classified into 7 groups: uninfected untreated (I), infected untreated (II), infected treated orally with PZQ (1,000 mg/kg) (III), QN (400 mg/kg) (IV), KTZ (10 mg/kg) +QN as group IV (V), HF (400 mg/kg) (VI), and KTZ (as group V) +HF (as group VI) (VII) . KTZ plus QN or HF produced more inhibition (P<0.05) in hepatic CYP450 (85.7% and 83.8%) and CYT b5 (75.5% and 73.5%) activities, respectively, than in groups treated with QN or HF alone. This was accompanied with more reduction in female (89.0% and 79.3%), total worms (81.4% and 70.3%), and eggs burden (hepatic; 83.8%, 66.0% and intestinal; 68%, 64.5%), respectively, and encountering the granulomatous reaction to parasite eggs trapped in the liver. CYP24A1 inhibitor enhances antiproliferative effects, increases systemic calcitriol exposure, and promotes the activation of caspase-independent apoptosis pathway. Ketoconazole is also a potent exosome biogenesis and/or secretion inhibitor.

65277-42-1

R 41400

Pharmacology & Drug Discovery

>98% (HPLC)

Ethanol: 7 mg/mL (13.17 mM) ; DMSO: 3 mg/mL (5.64 mM)

CC (N1CCN (C2=CC=C (OC[C@@H]3O[C@@] (CN4C=CN=C4) (C5=CC=C (Cl) C=C5Cl) OC3) C=C2) CC1) =O

C26H28Cl2N4O4

531.43

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.