405098-33-1
405098-33-1 结构式
基本信息
化合物W-54011
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
CS-2062
C5a Receptor Antagonist, W-54011
N-{[4-(diMethylaMino)phenyl]Methyl}-7-Methoxy-N-[4-(propan-2-yl)phenyl]-1,2,3,4-tetrahydronaphthalene-1-carboxaMide hydrochloride
N-[[4-(DIMETHYLAMINO)PHENYL]METHYL]-1,2,3,4-TETRAHYDRO-7-METHOXY-N-[4-(1-METHYLETHYL)PHENYL]-1-NAPHTHALENECARBOXAMIDE HYDROCHLORIDE
常见问题列表
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. |