中文名称: ZD-1611
英文名称: ZD-1611
CAS No: 186497-38-1
分子式: C22H24N4O5S
分子量: 456.51
Z10063 ZD-1611 (psaitong)
包装规格:
100mg in glass bottle
产品描述:

基本信息

产品编号:Z10063

产品名称:ZD-1611

CAS:

186497-38-1

 

储存条件

粉末

-20℃

四年

分子式:

C22H24N4O5S

溶于液体

-80℃

两年

分子量:

456.51

 

 

化学名: 

 

 

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。

 

生物活性

产品描述

一种有效的,可口服的,选择性的 ETA receptor 拮抗剂,可用于缺血性脑中风的研究。

靶点/IC50

Endothelin Receptor

 

体外研究

ZD1611 competitively inhibits 125I-labeled ET-1 binding at human cloned ETA and ETB receptors with pIC50 values of 8.6 and 5.6, respectively, showing 1000-fold selectivity for the ETA receptor.

体内研究

ZD1611 (0.3mg/kg,p.o.) has a duration of action of more than 7h in rats. In the dog,ZD1611 is active for at least 6h at dose of 0.6mg/kg p.o.ZD1611 (0.15mg/kg/day) in combination with candesartan decreases the brain damage and improves the neurological scores in rats.However,ZD1611 or candesartan alone does not significantly decrease the brain damage or improve neurological scores.

 

推荐实验方法(仅供参考)

动物实验:

 

The precursor of ET-1,big ET-1,is used for in vivo analysis of the effects of ZD1611.Exogenously administered big ET-1 is converted to the biologically active peptide ET-1 in vivo via a phosphoramidon-sensitive ET-converting enzyme.In the present study,the use of big ET-1 in vivo is preferred because this compound fails to elicit the initial depressor response associated with i.v.administered ET-1 and yields a greater maximum response than that to ET-1 itself.A partial cumulative dose-response curve to i.v.big ET-1 starting at 0.3nmol/kg) is constructed until pressor responses >30 mm Hg are achieved.After a 55-min recovery period,ZD1611 (0.03-0.3mg/kg) or vehicle is administered,and the big ET-1-response curve is repeated 5 min later.The activity of ZD1611 is calculated as a ratio of the dose of big ET-1 required to give a 30-mm Hg rise in MAP in the absence and then the presence of the compound.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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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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连续稀释计算器方程

  • 连续稀释

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  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    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):