W-54011

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 (Ki = 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, Cay-21495), 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).Formal Name: N-[[4-(dimethylamino)phenyl]methyl]-1,2,3,4-tetrahydro-7-methoxy-N-[4-(1-methylethyl)phenyl]-1-naphthalenecarboxamide, monohydrochloride. CAS Number: 405098-33-1. Molecular Formula: C30H36N2O2 . HCl. Formula Weight: 493.1. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: :, DMF: 30 mg/mL, DMSO: 30 mg/mL, Ethanol: 3 mg/mL. lambdamax: 263 nm. SMILES: CN(C)C1=CC=C(CN(C(C2CCCC3=C2C=C(OC)C=C3)=O)C4=CC=C(C(C)C)C=C4)C=C1.Cl. InChi Code: InChI=1S/C30H36N2O2.ClH/c1-21(2)23-11-16-26(17-12-23)32(20-22-9-14-25(15-10-22)31(3)4)30(33)28-8-6-7-24-13-18-27(34-5)19-29(24)28,/h9-19,21,28H,6-8,20H2,1-5H3,1H. InChi Key: UKBJWRMNGCDKNL-UHFFFAOYSA-N.