14α-demethylase

Itraconazole (R51211) 属于三唑类天然产物，是一种抗真菌剂，具有口服活性。Itraconazole 是一种 Hedgehog 信号通路拮抗剂，一种 oxysterol-binding protein (OSBP) 抑制剂，也是一种细胞色素 P-450 依赖性酶的抑制剂。

14α-Demethylase DNA Gyrase-IN-2 (Compound 6a) 是一种 14α-Demethylase DNA Gyrase 的有效抑制剂，具有抗菌作用。

14α-Demethylase DNA Gyrase-IN-1 (Compound 7c) 是一种 14α-Demethylase DNA Gyrase 的有效抑制剂，具有抗菌作用。

14α-Demethylase-IN-1 (compound 2e) 作为一种14α-demethylase抑制剂，主要用于抗真菌治疗。在抑制不同类型的念珠菌上，其表现出不同的最小抑菌浓度 (MIC50) 值。具体而言，对白色念珠菌、近平滑念珠菌、克柔念珠菌及光滑念珠菌的MIC50值在48小时内分别达到2.47 μM、1.23 μM、19.70 μM 和 19.70 μM。

PC945 (Opelconazole) 是一种有效的广谱抗真菌化合物，对烟曲霉甾醇 14α-去甲基酶 (CYP51A CYP51B) 有抑制作用，可用于研究肺部真菌感染。

Antifungal agent 40 是抗真菌剂，能够延伸到 C.alb.CYP51 的狭窄疏水口袋 II 中，可抑制 lanosterol 14α-demethylase (CYP51) 的活性，对生物膜的形成具有抑制作用。

Antifungal agent 42 是一种抗真菌剂，对生物膜形成具有抑制作用。Antifungal agent 42 能够抑制 C.alb.的 lanosterol 14α-demethylase (CYP51)。

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

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.

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.

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......

Antifungalagent 68（compound 10）是抗真菌剂，针对念珠菌和格特隐球菌。它通过抑制麦角甾醇的生物合成发挥作用，靶向羊毛甾醇 14α-去甲基酶（CYP51）。Antifungalagent 68的咪唑环能与CYP51的血红素基团发生相互作用。