| Identification | Back Directory | [Name]
Factor D inhibitor 6 | [CAS]
1386455-51-1 | [Synonyms]
Factor D inhibitor 6
2-Azabicyclo[3.1.0]hexane-3-carboxamide, 2-[2-[3-(aminocarbonyl)-1H-pyrazolo[3,4-c]pyridin-1-yl]acetyl]-N-[(1R)-1-(3-chloro-2-fluorophenyl)ethyl]-, (1R,3S,5R)- | [Molecular Formula]
C23H22ClFN6O3 | [MOL File]
1386455-51-1.mol | [Molecular Weight]
484.91 |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [storage]
Store at -20°C | [References]
[1]. Jürgen Maibaum, et al. Small-molecule Factor D Inhibitors Targeting the Alternative Complement Pathway. Nat Chem Biol. 2016 Dec;12(12):1105-1110. |
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