W-54011? , ≥98% , 405098-33-1

Synonym(s):
C5a Receptor Antagonist, W-54011 - CAS 405098-33-1 - Calbiochem;N-((4-Dimethylaminophenyl)methyl)-N-(4-isopropylphenyl)-7-methoxy-1,2,3,4-tetrahydronaphthalen-1-carboxamide, HCl

CAS NO.：405098-33-1

Empirical Formula: C30H37ClN2O2

Molecular Weight: 493.08

MDL number: MFCD06659046

PRODUCT Properties

• storage temp.: Store at -20°C
• solubility: DMF: 30 mg/mL; DMSO: 30 mg/mL; Ethanol: 3 mg/mL
• form: White powder solid.
• color: White to light yellow
• Stability: Hygroscopic

Description and Uses

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.