W-54011 is an orally bioavailable, nonpeptide antagonist of complement component 5a receptor 1 (C5aR), also known as cluster of differentiation 88 (CD88).
1 W-54011 inhibits
125I-rhC5a binding in neutrophils (K
i = 2.2 nM) and C5a-mediated intracellular Ca
2+ mobilization (IC
50 = 3.1 nM).
1 W-54011 is selective and does not affect Ca
2+ 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.
1 It inhibits Ca
2+ mobilization in neutrophils in humans, cynomolgus monkeys, and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs.
1 At 10 nM, W-54011 also inhibits C5a-mediated migration and vessel formation of human microvascular endothelial cells (HMEC-1).
2 
