Formulation: A solid
Formal Name: (2R,3S)-2-[4-(cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl-3-(trifluoromethyl)phenyl]-3-piperidinecarboxamide
Purity: ≥95% (mixture of isomers)
Formula Markup: C33H35F4N3O2
Formula Weight: 581,6
Shelf life (days): 1460
CAS Number: 1346623-17-3
Notes: Avacopan is an antagonist of the complement 5a1 (C5a1) receptor (IC50 = 0.1 nM).{64646} It is selective for C5a1 over the C5a2 receptor and chemokine-like receptor 2 (CMKLR2), also known as chemerin receptor 2 or GPR1 (IC50s = >10,000 nM for both), as well as the C3a receptor, CMKLR1, and formyl peptide receptor 1 (FPR1; IC50s = >10,000 nM for all), and over panels of 18 chemokine receptors (IC50s = ≥6,700 nM for all), 54 other receptors at 10 µM, and five cytochrome P450 (CYP) isoforms (IC50s = >10,000 nM for all). Avacopan (50 nM) reduces the migration of isolated cynomolgus monkey neutrophils. It also reduces C5a-induced increases in neutrophil cell surface levels of CD11b in whole blood isolated from mice with a knock-in of human C5AR1, the gene encoding the C5a1 receptor, when used at concentrations of 10 and 100 nM or when administered at doses of 0.075 or 0.15 mg/kg. Formulations containing avacopan have been used in the adjunctive treatment of severe vasculitis associated with anti-neutrophil cytoplasmic autoantibodies (ANCA).
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