中文名称: | ZD-1611 | ||||
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英文名称: | ZD-1611 | ||||
CAS No: | 186497-38-1 | 分子式: | C22H24N4O5S | 分子量: | 456.51 |
CAS No: | 186497-38-1 | ||||
分子式: | C22H24N4O5S | ||||
分子量: | 456.51 |
基本信息
产品编号:Z10063 |
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产品名称:ZD-1611 |
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CAS: |
186497-38-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃ |
两年 |
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分子量: |
456.51 |
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化学名: |
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Solubility (25°C) |
体外 |
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。 |
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: |
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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. |
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 )