Posaconazole hydrate_C14ɑ去甲基化酶抑制剂_1198769-38-8_Apexbio

产品名: Posaconazole hydrate 修订日期: 6/30/2016产品说明书

化学性质

产品名:

Posaconazole hydrate

Cas No.:

1198769-38-8 分子量:

718.79 分子式: C37H44F2N8O5

化学名: 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorop

henyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-1

-((2S,3S)-2-hydroxypentan-3-yl)-1H-1,2,4-triazol-5(4H)-one hydrate

SMILES: CC[C@@](N(N=CN1C2=CC=C(N3CCN(C4=CC=C(OC[C@@](CO5)([H])

C[C@@]5(C6=C(F)C=C(F)C=C6)CN7C=NC=N7)C=C4)CC3)C=C2)C1=O)(

[H])[C@](O)([H])C.O

溶解性: Soluble in DMSO

储存条件: Store at -20°C

一般建议: For obtaining a higher solubility , please warm the tube at 37°C

and shake it in the ultrasonic bath for a while.Stock solution can be

stored below -20°C for several months.

运输条件:

Evaluation sample solution : ship with blue ice

All other available size: ship with RT , or blue ice upon request

生物活性

靶点 :

Metabolism 信号通路:

C14ɑ demethylase 产品描述:

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 C14ɑdemethylase 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.

参考文献:

特别声明

产品仅用于研究，

不针对患者销售，望谅解。

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