中文名称: | A-192621 | ||||
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英文名称: | A-192621 | ||||
CAS No: | 195529-54-5 | 分子式: | C33H38N2O6 | 分子量: | 558.66 |
CAS No: | 195529-54-5 | ||||
分子式: | C33H38N2O6 | ||||
分子量: | 558.66 |
基本信息
产品编号: |
A11292 |
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产品名称: |
A-192621 |
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CAS: |
195529-54-5 |
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: |
558.66 |
-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 |
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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 |
一种有效的非肽,口服活性,选择性内皮素B (ETB)受体拮抗剂,IC50为 4.5nM,Ki为8.8nM。 |
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靶点 |
Endothelin Receptor |
Apoptosis |
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体外研究 |
A-192621 (1-100μM;48 hours;PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner.A-192621 (1-100μM;48 hours;PASMCs) treatment significantly increases the caspase-3/7 activity and cleaved caspase-3 expression in PASMCs.A-192621 induces apoptosis in a dose-dependent manner and increases the cells' susceptibility to apoptosis by Doxorubicin treatment. Cell Viability Assay |
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Cell Line: |
Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin |
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Concentration: |
1μM,10μM,50μM,100μM |
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Incubation Time: |
72 hours |
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Result: |
The viability of PASMCs was significantly decreased in a dose-dependent manner. |
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Western Blot Analysis |
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Cell Line: |
Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin |
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Concentration: |
1μM,10μM,100μM |
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Incubation Time: |
72 hours |
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Result: |
The caspase-3/7 activity in PASMCs was significantly increased in a dose-dependent manner. |
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体内研究 |
A-192621 (30-100mg/kg;oral administration;daily;for 3 days;male Sprague-Dawley rats) treatment inhibits both dilatory and pressor responses induced by S6c mediated by ETB with an ED50 value of 30mg/kg,and failed to inhibit the ET-1-induced pressor response mediated by ETA.A-192621 alone causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level in the conscious normotensive rat. |
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Animal Model: |
Male Sprague-Dawley rats (250-350g) |
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Dosage: |
30mg/kg 100mg/kg |
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Administration: |
Oral administration;daily;for 3 days |
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Result: |
Inhibited both dilatory and pressor responses induced by S6c mediated by ETB with an ED 50value of 30mg/kg. |
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 )