中文名称: | W-54011 | ||||
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英文名称: | W-54011 | ||||
别名: | N-[[4-(dimethylamino)phenyl]methyl]-7-methoxy-N-(4-propan-2-ylphenyl)-1,2,3,4-tetrahydronaphthalene-1-carboxamide | ||||
CAS No: | 405098-33-1 | 分子式: | C30H37ClN2O2 | 分子量: | 493.08 |
CAS No: | 405098-33-1 | ||||
分子式: | C30H37ClN2O2 | ||||
分子量: | 493.08 |
基本信息
产品编号: |
W10070 |
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产品名称: |
W-54011 |
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CAS: |
405098-33-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
493.08 |
-20℃ |
1个月 |
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化学名: |
N-[[4-(dimethylamino)phenyl]methyl]-7-methoxy-N-(4-propan-2-ylphenyl)-1,2,3,4-tetrahydronaphthalene-1-carboxamide |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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靶点 |
Ki:2.2nM (C5a)sup> IC50:3.1nM (Ca2+ mobilization),2.7nM (Chemotaxis),and 1.6nM (ROS) |
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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. |
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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. |
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Animal Model: |
Male mongolian gerbils (6-12 weeks) injected with rhC5a |
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Dosage: |
3mg/kg,10mg/kg,30mg/kg |
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Administration: |
Oral administration;for 4 hours |
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Result: |
Inhibited C5a-induced neutropenia in a dose-dependent manner. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )