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Danicopan
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。
Danicopan图片
CAS NO:1903768-17-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议

产品介绍
Danicopan (ACH-4471) 是一种选择性的口服活性 small-molecule factor D 抑制剂,对 small-molecule factor D 具有高结合亲和力,其 Kd 值为 0.54 nM。Danicopan (ACH-4471) 可抑制补体 (APC) 活性的替代途径,具有阻断阵发性夜间血红蛋白尿 (PNH) 和非典型溶血性尿毒症综合征(aHUS) 的补体替代途径的潜力。
Cas No.1903768-17-1
别名ACH-4471
Canonical SMILESO=C([C@H]1N(C(CN2N=C(C(C)=O)C3=C2C=CC(C4=CN=C(C)N=C4)=C3)=O)C[C@H](F)C1)NC5=NC(Br)=CC=C5
分子式C26H23BrFN7O3
分子量580.41
溶解度DMSO: 260 mg/mL (447.96 mM)
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

Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS)[1].

Danicopan (ACH-4471) inhibits the proteolytic activity of purified Factor D against its natural substrate Factor B in complex with C3b, blocking production of Bb fragment in a dose-dependent manner with an IC50 value of 0.015 μM[1].Danicopan (ACH-4471)potently inhibits hemolysis with IC50 values ranging from 0.0040 μM to 0.027 μM (IC90 values from 0.015 μM to 0.11 μM) [1].

[1]. Yuan X, et al. Small-molecule factor D inhibitors selectively block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria and atypical hemolytic uremic syndrome. Haematologica. 2017 Mar;102(3):466-475.