Factor D inhibitor 6

Research use only, not for human use.

Factor D inhibitor 6 is a potent and selective, orally bioavailable inhibitor of Factor D with IC50 of 30 nM.

Factor D inhibitor 6 is a potent and selective, orally bioavailable inhibitor of Factor D with IC50 of 30 nM; is highly selective for human FD, showing no inhibition of factor B; efficiently block alternative pathway activation and prevent both C3 deposition onto, and lysis of, PNH erythrocytes; inhibits lipopolysaccharide-induced AP activation in FD-humanized mice.

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.

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. 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.

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Immunology/Inflammation

Complement System

Complement System

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1386455-51-1

484.916

C23H22ClFN6O3

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (515.56 mM)

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1-(2-((1R,3S,5R)-3-(((R)-1-(3-chloro-2-fluorophenyl)ethyl)carbamoyl)-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)-1H-pyrazolo[3,4-c]pyridine-3-carboxamide

(-20℃)

With Ice Pack

≥ 2 years