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-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。

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。

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。

(Rac)-Ketoconazole ((Rac)-R 41400) 是一种具有口服活性的抗真菌咪唑类化合物。通过抑制真菌细胞膜上关键的细胞色素 P450 依赖的 14α-甾醇去甲基化酶 (CYP51)，(Rac)-Ketoconazole 阻碍了真菌麦角固醇的合成，从而破坏细胞膜的功能，最终抑制真菌的生长和繁殖。该化合物可用于真菌感染的研究。

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。

Pyrisoxazole (Standard) is the standard substance of Pyrisoxazole, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Pyrisoxazole is a novel fungicide inhibitor of Sterol 14α-demethylase.