112559-91-8

• 常用中文名：羟基伊曲康唑
• 常用英文名：Hydroxy Itraconazole
• CAS号：112559-91-8
• 分子式：C₃₅H₃₈Cl₂N₈O₅
• 分子量：721.63
• 相关类别： 信号通路 抗感染 真菌
• 发布时间：2018-07-26 17:59:33
• 更新时间：2026-07-09 16:57:17
• Itraconazole metabolite Hydroxy Itraconazole 是 Itraconazole (ITZ) 的活性代谢物,Itraconazole 是一种三唑类抗真菌剂。

名称

• 中文名: 羟基伊曲康唑(伊曲康唑代谢物)
• 英文名: Hydroxy Itraconazole
• 中文别名: 4-(4-(4-((2-((1H-1,2,4-三唑-1-基)甲基)-2-(2,4-二氯苯基)-1,3-二氧戊环-4-基)甲氧基)苯基)哌嗪-1-基)苯基-2-(3-羟基丁-2-基)-2,4-二氢-3H-1,2,4-三唑-3-酮; 羟基四康唑; 羟基曲康唑; 伊曲康唑杂质8(羟基伊曲康唑); 伊曲康唑代谢物; 伊曲康唑杂质8; 伊曲康唑2-羟基代谢物; 羟基伊曲康唑/精确称量; 伊曲康唑杂质1; 羟基基伊曲康唑; 羟基伊曲康唑(非对映体混合物); 2H6]-羟基曲康唑; 依曲康唑杂质; 酮康唑杂质36
• 英文别名: Itraconazole 2-Hydroxy Metabolite; Itraconazole Impurity 8(Hydroxy Itraconazole); 4-(4-(4-(4-((2-((1H-1,2,4-Triazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-(3-hydroxybutan-2-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one; 4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-(3-hydroxybutan-2-yl)-1,2,4-triazol-3-one; 4-[4-[4-[4-[[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(2-hydroxy-1-methylpropyl)-3H-1,2,4-triazol-3-one; Itraconazole Impurity 1; Ketoconazole Impurity 36; 2H6]-Hydroxyitraconazole; Itraconazole metabolite Hydroxy Itraconazole; HYDROXY ITRACONAZOLE; Hydroxy ItraconazoleQ: What is Hydroxy Itraconazole Q: What is the CAS Number of Hydroxy Itraconazole Q: What is the storage condition of Hydroxy Itraconazole Q: What e the applications of Hydroxy Itraconazole; Hydroxy Itraconazole D8Q: What is Hydroxy Itraconazole D8 Q: What is the CAS Number of Hydroxy Itraconazole D8 Q: What is the storage condition of Hydroxy Itraconazole D8 Q: What e the applications of Hydroxy Itraconazole D8; 3H-1,2,4-Triazol-3-one, -2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-(2-hydroxy-1-methylpropyl); 4-[4-[4-[4-[[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylMethyl)-1,3-dioxolan-4-yl]Methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(2-hydroxy-1-Methylpropyl); Hydroxy Itraconazole (10mM in DMSO); Hydroxy Itraconazole (Itraconazole metabolite Hydroxy Itraconazole

物化性质

• 密度: 1.44g/cm3
• 沸点: 884.7ºC at 760mmHg
• 熔点: 76-78ºC
• 分子式: C₃₅H₃₈Cl₂N₈O₅
• 分子量: 721.63
• 闪点: 488.8ºC
• PSA: 103.95000
• LogP: 4.96710
• 蒸汽压: 0mmHg at 25°C
• 折射率: 1.687
• 储存条件: 2-8℃

生物活性

• 描述: Itraconazole metabolite Hydroxy Itraconazole 是 Itraconazole (ITZ) 的活性代谢物,Itraconazole 是一种三唑类抗真菌剂。
• 相关类别:
  信号通路 >> 抗感染 >> 真菌
  研究领域 >> 其他
• 靶点:

  Antifungal[1]

• 体外研究: 羟基伊曲康唑(OH-ITZ)是伊曲康唑(ITZ)的活性代谢产物。虽然据报道OH-ITZ在体外具有抗真菌活性,但其在人体内的药代动力学研究较少于ITZ。 ITZ和OH-ITZ具有三唑环并抑制CYP3A。与单次给药相比,重复给药可使其半衰期延长26-60％[1]。
• 体内研究: OH-ITZ的血浆浓度很弱地取决于ITZ的剂量,很可能是因为形成OH-ITZ的过程是饱和的。血清白蛋白和GFR可改变ITZ和OH-ITZ的药代动力学。应该讨论抗真菌活性,同时不仅要考虑ITZ的血浆浓度,还要考虑OH-ITZ的血浆浓度。然而,在服用ITZ口服溶液的免疫受损患者中,OH-ITZ的药代动力学类似于ITZ的药代动力学。由于ITZ和OH-ITZ的血浆浓度密切相关,从临床角度来看,确定血浆中任一种的浓度应该是足够的[1]。
• 参考文献:

  [1]. Mino Y, et al. Hydroxy-itraconazole pharmacokinetics is similar to that of itraconazole in immunocompromised patients receiving oral solution of itraconazole. Clin Chim Acta. 2013 Jan 16;415:128-32.