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，K_d 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。

Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC 50 of 30 nM and a K d 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.

Solid

IC50: 30 nM (Factor D)
Kd: 6 nM (Factor D)

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).
Factor D inhibitor 6 (compound 6) shows modest inhibition of murine FD (IC50 = 0.86 μM).
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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

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

In Vitro: DMSO : 250 mg/mL (515.56 mM; Need ultrasonic)配制储备液