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W-54011  ≥98%

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包装规格：1mg 5mg 10mg 50mg in glass bottle
溶解性：溶于DMSO(≥28mg/mL）
产品描述：基本信息 产品编号： W10070 产品名称： W-54011 CAS: 405098-33-1   储存条件 粉末 -20℃ 四年     分子式： C30H37ClN2O2 溶于液体 -80℃ 6个月 分子量： 493.08 -20℃ 1个月 化学名：  N-[[4-(dimethylamino)phenyl]methyl]-7-methoxy-N-(4-propan-2-ylphenyl)-1,2,3,4-tetrahydronaphthalene-1-carboxamide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.0281mL 10.1403mL 20.2807mL 5mM 0.4056mL 2.0281mL 4.0561mL 10mM 0.2028mL 1.0140mL 2.0281mL   生物活性 产品描述 一种有效的，具有口服活性的非肽C5a受体拮抗剂。 靶点 Ki:2.2nM (C5a)sup> IC50:3.1nM (Ca2+ mobilization),2.7nM (Chemotaxis),and 1.6nM (ROS)   体外研究 In C5a-induced intracellular Ca2+ mobilization assay with human neutrophils,W-54011 does not show agonistic activity at up to 10μM 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 10μM,W-54011 does not affect Ca2+ mobilization stimulated with sub-maximally effective concentrations of fMLP (1nM),plateletactivating factor (0.3nM),and IL-8 (0.1nM).This result demonstrates that W-54011 is highly specific for C5a receptor. 体内研究 W-54011 (3-30mg/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 Ca2+ mobilization of neutrophils in various species.The W-54011 is able to inhibit the response in cynomolgus monkeys and gerbils with IC50 values of 1.7nM and 3.2nM,respectively,but not in mice,rats,guinea pigs,rabbits,and dogs. Animal Model: Male mongolian gerbils (6-12 weeks) injected with rhC5a Dosage: 3mg/kg,10mg/kg,30mg/kg Administration: Oral administration;for 4 hours Result: Inhibited C5a-induced neutropenia in a dose-dependent manner.
保存条件：-20℃

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