Factor D inhibitor 6

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 In Vitro 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). Factor D inhibitor 6 (compound 6) shows modest inhibition of murine FD (IC 50 = 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 IC 50 value of 70 nM, consistent with inhibition of the AP amplification loop. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57Bl/6 mice induced by lipopolysaccharide (LPS) 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. IC50& Target:IC50: 30 nM (Factor D), Kd: 6 nM (Factor D)

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