| Name | W-54011 |
| 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 neutrophils (IC50s = 3.1 nM, 2.7 nM, and 1.6 nM, respectively). |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.06 mM), Sonication is recommended.
DMSO : 28 mg/mL (56.79 mM), Sonication is recommended.
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| Keywords | W-54011 | W54011 | W 54011 | ROS | Reactive Oxygen Species | orally | neutrophils | mobilization | Inhibitor | inhibit | inflammatory | ComplementSystem | Complement System | complement 5a receptor (C5aR) | chemotaxis | Ca2+ mobilization, | Ca2+ | C5a | anaphylatoxin |
| Inhibitors Related | Ethoxyquin | Kaolin | Allopurinol | Cysteamine hydrochloride | Ethyl linoleate | Magnesium acetate tetrahydrate | Inosine | L-Cystine | Copper Sulfate Pentahydrate | L-Ascorbic acid sodium salt | Dimethyl phthalate | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Ferroptosis Compound Library | NF-κB Signaling Compound Library | Bioactive Compound Library | HIF-1 Signaling Pathway Compound Library | Antioxidant Compound Library | Inhibitor Library | Mitochondria-Targeted Compound Library | Metabolism Compound Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
