W-54011

• CAT Number: I003473
• CAS Number: 405098-33-1
• Molecular Formula: C30H36N2O2 • HCl
• Molecular Weight: 493.1
• Purity: ≥95%
• Synonyms: N-[[4-(dimethylamino)phenyl]methyl]-1,2,3,4-tetrahydro-7-methoxy-N-[4-(1-methylethyl)phenyl]-1-naphthalenecarboxamide, monohydrochloride
• Target: NF-κB
• Solubility: DMSO: ＜ 8.4 mg/mL
• Storage: -20°C
• IC50: 2.2 nM (Ki)
• IUPAC Name: N-[[4-(dimethylamino)phenyl]methyl]-7-methoxy-N-(4-propan-2-ylphenyl)-1,2,3,4-tetrahydronaphthalene-1-carboxamide;hydrochloride
• InChI: 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
• InChIKey: UKBJWRMNGCDKNL-UHFFFAOYSA-N
• SMILES: CC(C)C1=CC=C(C=C1)N(CC2=CC=C(C=C2)N(C)C)C(=O)C3CCCC4=C3C=C(C=C4)OC.Cl

W-54011(CAT: I003473) is a potent and orally active CD88 (C5a receptor) antagonist. It selectively inhibits the binding of C5a to CD88, blocking C5a-induced intracellular Ca2+ mobilization, chemotaxis, and reactive superoxide species generation in human neutrophils. With its species-specific activity in gerbils and cynomolgus monkeys, W-54011 shows promise as a non-peptide C5a receptor antagonist for the treatment of inflammatory diseases mediated by C5a. The compound’s pharmacologic action involves targeting CD88, and its potential applications include the development of therapies aimed at modulating the effects of C5a in various disease conditions.

Overview of Clinical Research

W-54011 is a complement C5a inhibitor. Preclinical trials was initiated in Inflammation in Japan (unspecified route) in 2003.

Reference

1. Sumichika H, et al. Identification of a potent and orally active non-peptide C5a receptor antagonist. J Biol Chem. 2002 Dec 20;277(51):49403-49407.