| 中文名称: | Sparsentan | ||||
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| 英文名称: | Sparsentan | ||||
| 别名: | RE-021; DARA-a | ||||
| CAS No: | 254740-64-2 | 分子式: | C32H40N4O5S | 分子量: | 592.75 |
| CAS No: | 254740-64-2 | ||||
| 分子式: | C32H40N4O5S | ||||
| 分子量: | 592.75 | ||||
基本信息
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产品编号： |
S10848 |
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产品名称： |
Sparsentan |
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CAS: |
254740-64-2 |
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： |
592.75 |
-20℃ |
1个月 |
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化学名： |
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Solubility (25°C)： |
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体外:
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DMSO |
100mg/mL (168.7mM) |
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Ethanol |
40mg/mL (67.48mM) |
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Water |
Insoluble |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
1.6871mL |
8.4353mL |
16.8705mL |
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5mM |
0.3374mL |
1.6871mL |
3.3741mL |
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10mM |
0.1687mL |
0.8435mL |
1.6871mL |
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50mM |
0.0337mL |
0.1687mL |
0.3374mL |
生物活性
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产品描述 |
一种高度选择的血管紧张素 II (angiotensin II) 和内皮素 A (endothelin A) 受体的双重拮抗剂，Ki 值分别为 0.8 和 9.3nM。 |
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靶点 |
Ki:0.8nM (Human angiotensin II),9.3nM (Human endothelin A),0.4nM (Rat angiotensin II) |
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体内研究 |
Sparsentan dose dependently antagonizes the angiotensin II-induced pressor response with an ED50 value of 0.8µmol/kg iv and 3.6µmol/kg po.Sparsentan also shows efficacious and long acting in the big ET-1-induced pressor model.Sparsentan causes a significant lowering of blood pressure at the lowest dose tested (10µmol/kg/day) in spontaneously hypertensive rats.Sparsentan shows good oral bioavailability in rats,dogs,and monkeys, averaging 40%,86%,and 21% F,respectively.At 100µmol/kg/day,Sparsentan reduces the blood pressure from 170 to less than 100mmHg during the course of the drug’s pharmacokinetic duration.Sparsentan at 100µmol/kg/day essentially converts the spontaneously hypertensive rats into normotensive rats during the course of its pharmacokinetic duration. |
推荐实验方法(仅供参考)
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动物实验: |
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Rats:Rats are gavaged with vehicle,and immediately thereafter the first bolus (intravenous) iv injection of angiotensin II served as the control pressor response.Irbesartan (30µmol/kg) and Sparsentan (30µmol/kg) are given by oral gavage (po),and the rats are re-challenged with angiotensin II at various intervals up to 240 min.There are 6-8 rats per drug dose.The difference between the maximum blood pressure increase before and after drug is reported as the percent (%) inhibition of the angiotensin II pressor effect. |
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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 )
