产品说明书
IRL 2500
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同义名 : | - |
| CAS号 : | 169545-27-1 | |
| 货号 : | A885645 | |
| 分子式 : | C36H35N3O4 | |
| 纯度 : | 98%+ | |
| 分子量 : | 573.681 | |
| MDL号 : | MFCD00948945 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(183.03 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The ETB receptor is expressed on vascular endothelial cells where it induces endothelial-dependent vasodilatation through NO production and clearance of circulating ET-1[1]. IRL 2500, a potent endothelin receptor antagonist, inhibits the binding of [125I]-endothelin-1 (ET-1) to human ETB (IC50 1.3 ± 0.2 nM) and ETA (IC50 94 ± 3 nM) receptors expressed in transfected Chinese hamster ovary (CHO) cells. In in vitro studies, IRL 2500 inhibited the sarafotoxin S6c (STX6c)-mediated contraction of the dog saphenous vein (pKb 7.77) and the STX6c-induced relaxation of the preconstricted rabbit mesenteric artery (pKb 6.92). In the anesthetized rat, IRL 2500 (10 mg/kg, i.v.) inhibited the initial transient decrease in mean arterial pressure (MAP) induced by the ETB-selective agonist IRL 1620 (0.5 nmol/kg, i.v.). IRL 2500 also attenuated the IRL 1620-mediated increase in renal vascular resistance (RVR) in the anesthetized rat[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.74mL 0.35mL 0.17mL |
8.72mL 1.74mL 0.87mL |
17.43mL 3.49mL 1.74mL |
| 参考文献 |
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