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Hydroxy Itraconazole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Hydroxy Itraconazole图片
CAS NO:112559-91-8
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议

产品介绍
Hydroxy Itraconazole (Itraconazole metabolite Hydroxy Itraconazole; R-63373) 是 Itraconazole (ITZ) 的活性代谢物,它是一种三唑类抗真菌剂。
Cas No.112559-91-8
别名羟基伊曲康唑; Itraconazole metabolite Hydroxy Itraconazole; R-63373
Canonical SMILESO=C1N(C(C)C(O)C)N=CN1C2=CC=C(N3CCN(C4=CC=C(OCC5OC(CN6N=CN=C6)(C7=CC=C(Cl)C=C7Cl)OC5)C=C4)CC3)C=C2
分子式C35H38Cl2N8O5
分子量721.63
溶解度DMSO: 100 mg/mL (138.58 mM); Water:< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Hydroxy Itraconazole is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.

Hydroxy Itraconazole (OH-ITZ) is an active metabolite of Itraconazole (ITZ). Although Hydroxy Itraconazole is also reported to have antifungal activity in vitro, its pharmacokinetics in humans has been studied less than that of ITZ. ITZ and Hydroxy Itraconazole have a triazole ring and inhibit CYP3A. Their half-lives can be extended by 26-60% with repeated administration compared to single administration[1].

The plasma concentration of Hydroxy Itraconazole is weakly dependent on the dose of ITZ, most likely because the process that forms Hydroxy Itraconazole is saturated. Serum albumin and GFR may alter the pharmacokinetics of ITZ and Hydroxy Itraconazole. Antifungal activity should be discussed while taking into account not only the plasma concentration of ITZ but also that of Hydroxy Itraconazole. However, the pharmacokinetics of Hydroxy Itraconazole is similar to that of ITZ in immunocompromised patients taking an oral solution of ITZ. Since the plasma concentrations of ITZ and Hydroxy Itraconazole are closely correlated, determining the plasma concentration of either should be sufficient from a clinical point of view[1].

[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.