中文名称: W-54011
英文名称: W-54011
CAS No: 405098-33-1
分子式: C30H37ClN2O2
分子量: 493.08
W10070 W-54011 ≥98% (psaitong)
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℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
参考文献 & 客户发表文献

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

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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

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  • 计算结果

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):