W-54011
| 中文名称 | W-54011 |
|---|---|
| 中文同义词 | 化合物 T17250;N-(4-(二甲氨基)苄基)-N-(4-异丙基苯基)-7-甲氧基-1,2,3,4-四氢萘-1-甲酰胺盐酸盐;化合物W-54011;W 54011,C5A受体拮抗剂 |
| 英文名称 | N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE |
| 英文同义词 | N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE;N-{[4-(diMethylaMino)phenyl]Methyl}-7-Methoxy-N-[4-(propan-2-yl)phenyl]-1,2,3,4-tetrahydronaphthalene-1-carboxaMide hydrochloride;W-54011;C5a Receptor Antagonist, W-54011;CS-2062;chemotaxis,inhibit,orally,W-54011,mobilization,anaphylatoxin,ROS,Reactive Oxygen Species,Ca2+,C5a,neutrophils,Inhibitor,Complement System,W54011,inflammatory,W 54011;N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE |
| CAS号 | 405098-33-1 |
| 分子式 | C30H37ClN2O2 |
| 分子量 | 493.08 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 405098-33-1.mol |
| 结构式 |  |
W-54011 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | DMF：30mg/mL；二甲基亚砜：30mg/mL；乙醇：3mg/mL |
| 形态 | 白色粉末状固体。 |
| 稳定性 | 吸湿性 |
Ki: 2.2 nM (C5a)sup>[1]
IC50: 3.1 nM (Ca
2+
mobilization,), 2.7 nM (Chemotaxis), and 1.6 nM (ROS)
In C5a-induced intracellular Ca 2+ mobilization assay with human neutrophils, 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, indicating 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), plateletactivating factor (0.3 nM), and IL-8 (0.1 nM). This result demonstrates that W-54011 is highly specific for C5a receptor.
W-54011 (3-30 mg/kg; oral administration; for 4 hours; male mongolian gerbils) treatment inhibited C5a-induced neutropenia in a dose-dependent manner in gerbils.
The species selectivity of W-54011 is examined in rhC5a-induced intracellular Ca
2+
mobilization of neutrophils in various species. The W-54011 is able to inhibit the response in cynomolgus monkeys and gerbils with IC
50
values of 1.7 nM and 3.2 nM, respectively, but not in mice, rats, guinea pigs, rabbits, and dogs.
| Animal Model: | Male mongolian gerbils (6-12 weeks) injected with rhC5a |
| Dosage: | 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | Oral administration; for 4 hours |
| Result: | Inhibited C5a-induced neutropenia in a dose-dependent manner. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-16992A | W-54011 W-54011 | 405098-33-1 | 1mg | 900元 |
| 2024/01/25 | HY-16992A | W-54011 W-54011 | 405098-33-1 | 5mg | 1800元 |