产品描述:
W-54011 is an orally bioavailable, nonpeptide antagonist of complement component 5a receptor 1 (C5aR), also known as cluster of differentiation 88 (CD88).{34624} W-54011 inhibits 125I-rhC5a binding in neutrophils (Ki = 2.2 nM) and C5a-mediated intracellular Ca2+ mobilization (IC50 = 3.1 nM).{34624} 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; Item No. 21495), or IL-8 up to a concentration of 10 μM.{34624} It inhibits Ca2+ mobilization in neutrophils in humans, cynomolgus monkeys, and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs.{34624} At 10 nM, W-54011 also inhibits C5a-mediated migration and vessel formation of human microvascular endothelial cells (HMEC-1).{34625}