N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE

W 54011 is a potent orally active non-peptide C5a receptor antagonist.

W-54011 is an orally bioavailable, nonpeptide antagonist of complement component 5a receptor 1 (C5aR), also known as cluster of differentiation 88 (CD88). W-54011 inhibits ¹²⁵I-rhC5a binding in neutrophils (K_i = 2.2 nM) and C5a-mediated intracellular Ca²⁺ mobilization (IC₅₀ = 3.1 nM). W-54011 is selective and does not affect Ca²⁺ mobilization mediated by other G protein-coupled receptor (GPCR) ligands, N-Formyl-Met-Leu-Phe (fMLF; ), or IL-8 up to a concentration of 10 μM. It inhibits Ca²⁺ mobilization in neutrophils in humans, cynomolgus monkeys, and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs. At 10 nM, W-54011 also inhibits C5a-mediated migration and vessel formation of human microvascular endothelial cells (HMEC-1).

W 54011 is a potent orally active non-peptide C5a receptor antagonist.

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