14α-demethylase

14α-Demethylase DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase DNA Gyrase, exhibiting antibacterial activity.

14α-Demethylase DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase and DNA Gyrase, exhibiting significant antibacterial activity.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

PC945 (Opelconazole) is a potent broad-spectrum antifungal compound with inhibitory effect on fumonisinol 14α-demethylase (CYP51A CYP51B), which can be used in the study of fungal infections of the lungs.

Tebuconazole-d9 is intended for use as an internal standard for the quantification of tebuconazole by GC- or LC-MS. Tebuconazole is a triazole fungicide that is active against both seed and foliar fungi. It inhibits 14α-demethylase isolated from U. maydis and S. bicolor with IC50 values of 0.05 and 0.16 nM, respectively. It inhibits the androgenic effect of the androgen receptor agonist DHT (IC20 = 2.89 µM) and is cytotoxic (EC20 = 38.9 µM) in an MDA-kb2 assay. Tebuconazole (50 and 100 mg/kg per day) administered during gestation reduces testosterone levels and increases testicular levels of progesterone and 17α-hydroxyprogesterone in male rat fetuses. It has a feminizing effect on male pups and a virializing effect on female pups. When administered to rats gestationally through postnatal day 42, tebuconazole (20 and 60 mg/kg per day) leads to cell death of pyramidal cells in the CA3-4 region of the hippocampus and layer V of the cortex concomitant with impairment in learning......

Antifungal agent 68 (compound 10) effectively combats fungal infections caused by Candida and Cryptococcus gattii through the inhibition of ergosterol biosynthesis, likely via interaction with lanosterol 14α-demethylase (CYP51). The imidazole ring of antifungal agent 68 is proposed to interact with the heme group of CYP51 [1].

Antifungal agent 40 inhibits C. alb. CYP51 lanosterol 14α-demethylase (CYP51) by extending into the narrow hydrophobic pocket II, thereby affecting biofilm formation.

Pyrisoxazole is a novel fungicide inhibitor of Sterol 14α-demethylase.

Azalanstat mesylate is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat mesylate has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Antifungal agent 42 is an antifungal compound that inhibits biofilm formation and targets C.alb.'s lanosterol 14α-demethylase (CYP51).

Azalanstat HCl is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat HCl has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Tebuconazole is an agricultural azole fungicide. It can also inhibit CYP51 (IC50s: 0.9 and 1.3 μM for Candida albicans CYP51 and truncated Homo sapiens CYP51, respectively).

Itraconazole-d3 is a deuterated compound of Itraconazole.