产品描述
| 溶解性 |
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| 存贮条件 | 储存温度-20°C |
| 应用 | A triazole anti-fungal |
| 产品介绍 | Posaconazole 是甾醇C14ɑ去甲基化酶抑制剂，IC50为0.25 nM。 |
| 备注 | Posaconazole is a sterol C14ɑ demethylase inhibitor with an IC50 of 0.25 nM. |
| 生化机理 |
Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity. Posaconazole strongly inhibits 14-alpha demethylase, a cytochrome P450-dependent enzyme. Posaconazole is a sterol C14ɑ demethylase inhibitor with an IC50 of 0.25 nM. Inhibition of 14-alpha-demethylase prevents the conversion of lanosterol to ergosterol, an important component of the fungal cell wall. Inhibition of ergosterol synthesis changes the fungal cell membrane composition and integrity, alters membrane permeability and eventually leads to fungal cell lysis. Compared to other azole antifungals, posaconazole is a significantly more potent inhibitor of sterol 14-alpha demethylase. Posaconazole is the most advanced candidate for the treatment of Chagas disease. Posaconazole has entered in a phase II clinical trial in the treatment of mycoses. |
| 别名 | 泊沙康唑; 4-[4-[4-[4-[[(3R,5R)-5-(2,4-二氟苯基)-5-(1,2,4-三唑-1-基甲基)氧杂戊环-3-基]甲氧基]苯基]哌嗪-1-基]苯基]-2-[(2S,3S)-2-羟基戊-3-基]-1,2,4-三唑-3-酮;4-[4-[4-[4-[[(3R,5R)-5-(2,4-Difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one |
