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405098-33-1COc1ccc2c(c1)C(C(=O)N(Cc1ccc(N(C)C)cc1)c1ccc(C(C)C)cc1)CCC2.ClUKBJWRMNGCDKNL-UHFFFAOYSA-N405098-33-1DTXSID50415509CHEMBL5092226CHEBI:197423BeschreibungW-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; ), 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).
VerwendenW 54011 is a potent orally active non-peptide C5a receptor antagonist.
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