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W-54011 is a potent, specific, and orally active CD88 (C5a receptor) antagonist, which inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of reactive super oxide species in human neutrophils with IC50 alues of 3.1, 2.7, and 1.6 nM, respectively.
In vivo, in gerbils, oral administration of W-54011 (3-30 mg/kg) inhibits C5a-induced neutropenia in a dose-dependent manner. The present report is the first description of an orally active non-peptide C5a receptor antagonist that could contribute to the treatment of inflammatory diseases mediated by C5a.
| Molecular Weight | 493.08 |
| Formula | C30H37ClN2O2 |
| CAS Number | 405098-33-1 |
| Solubility (25°C) | DMSO: ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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