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Factor D inhibitor 6
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。
Factor D inhibitor 6图片
CAS NO:1386455-51-1
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
Factor D inhibitor 6 是一种有效的,高选择性,具有口服活性的因子 D (factor D) 抑制剂,IC50 为 30 nM,Kd 为 6 nM。Factor D inhibitor 6 对因子 B,激肽和凝集素补体途径激活以及广泛的受体,离子通道,激酶和蛋白酶等无活性。
Cas No.1386455-51-1
分子式C23H22ClFN6O3
分子量484.91
溶解度DMSO : 250 mg/mL (515.56 mM; Need ultrasonic)
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

Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases[1].

Factor D inhibitor 6 (compound 6) effectively blocks both alternative pathway (AP)-mediated hemolysis in 10% human serum (IC50 = 6 nM) and AP-induced membrane-attack complex (MAC) formation in lepirudinanticoagulated 50% human whole blood (IC50 = 0.14 μM)[1].Factor D inhibitor 6 (compound 6) shows modest inhibition of murine FD (IC50 = 0.86 μM)[1].Factor D inhibitor 6 (compound 6) inhibits both hemolysis and component 3 (C3) deposition on the surface of red blood cells (RBCs) with an IC50 value of 70 nM, consistent with inhibition of the AP amplification loop[1].

Factor D inhibitor 6 (Compound 6; 1-10 mg/kg; Oral gavage; once; C57Bl/6 mice) treatment dosed-ependently inhibits complement activation, with full inhibition at 10 mg/kg. Factor D inhibitor 6 shows sustained inhibition of LPS-induced AP activation for at least 8 h post-dose with an EC50 of 0.034 μM[1].

[1]. JÜrgen Maibaum, et al. Small-molecule Factor D Inhibitors Targeting the Alternative Complement Pathway. Nat Chem Biol. 2016 Dec;12(12):1105-1110.