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Factor D inhibitor 6

产品编号 T38803 CAS 1386455-51-1

Factor D inhibitor 6 is a potent, highly selective, orally active compound that specifically inhibits the activity of factor D (FD). It demonstrates an IC50 of 30 nM and a Kd of 6 nM. Notably, Factor D inhibitor 6 does not exhibit any inhibitory effects against factor B, classical and lectin complement-pathway activation, nor does it interfere with a broad array of receptors, ion channels, kinases, and proteases.

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Factor D inhibitor 6, CAS 1386455-51-1

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Factor D inhibitor 6 is a potent, highly selective, orally active compound that specifically inhibits the activity of factor D (FD). It demonstrates an IC50 of 30 nM and a Kd of 6 nM. Notably, Factor D inhibitor 6 does not exhibit any inhibitory effects against factor B, classical and lectin complement-pathway activation, nor does it interfere with a broad array of receptors, ion channels, kinases, and proteases.
靶点活性	FD:30 nM (IC50), FD:6 nM (Kd)
体外活性	Factor D inhibitor 6 (compound 6) effectively blocks both alternative pathway (AP)-mediated hemolysis in 10% human serum (IC 50 = 6 nM) and AP-induced membrane-attack complex (MAC) formation in lepirudinanticoagulated 50% human whole blood (IC 50 = 0.14 μM)[1]. Factor D inhibitor 6 (compound 6) shows modest inhibition of murine FD (IC 50 = 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 IC 50 value of 70 nM, consistent with inhibition of the AP amplification loop[1].
体内活性	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 EC 50 of 0.034 μM[1]. Animal Model: C57Bl/6 mice induced by lipopolysaccharide (LPS)[1]Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg Administration: Oral gavage; once Result: Dosed-ependently inhibited complement activation, with full inhibition at 10 mg/kg.

分子量	484.92
分子式	C23H22ClFN6O3
CAS No.	1386455-51-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

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

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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