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W-54011 is a potent non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils (Ki = 2.2 nM). W-54011 inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of ROS in human neutrophils (IC50s = 3.1 nM, 2.7 nM, and 1.6 nM, respectively).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 73 € | In Stock | |
5 mg | 122 € | In Stock | |
10 mg | 187 € | In Stock | |
25 mg | 335 € | In Stock | |
50 mg | 518 € | In Stock | |
100 mg | 747 € | In Stock | |
1 mL x 10 mM (in DMSO) | 159 € | In Stock |
Description | W-54011 is a potent non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils (Ki: 2.2 nM). W-54011 inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of ROS in human neutrophi |
Targets&IC50 | ROS:1.6 nM(ki), C5aR:2.2 nM(Ki), Ca2+ mobilization: 3.1 nM, Chemotaxis:2.7 nM(ki) |
In vitro | W-54011 does not show agonistic activity at up to 10 μM and shifts rightward the concentration-response curves to C5a without depressing the maximal responses, showing that W-54011 is a full antagonist. At concentrations up to 10 μM, W-54011 does not affect Ca2+ mobilization stimulated with sub-maximally effective concentrations of fMLP (1 nM), platelet-activating factor (0.3 nM), and IL-8 (0.1 nM)[1]. |
In vivo | W-54011 is able to inhibit the response in cynomolgus monkeys and gerbils (IC50 = 1.7 nM and 3.2 nM, respectively). In Male mongolian gerbils injected with rhC5a, W-54011 (3-30 mg/kg; oral; for 4 hours) inhibited C5a-induced neutropenia in a dose-dependent manner in gerbils. The species selectivity of W-54011 is examined in rhC5a-induced intracellular Ca2+ mobilization of neutrophils in various species [1]. |
Molecular Weight | 493.08 |
Formula | C30H37ClN2O2 |
Cas No. | 405098-33-1 |
Smiles | Cl.COc1ccc2CCCC(C(=O)N(Cc3ccc(cc3)N(C)C)c3ccc(cc3)C(C)C)c2c1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 28 mg/mL (56.79 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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