S88480 |
Darusentan |
| 源叶(MedMol) | 98% |
- 产品描述： Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM
- 靶点： Endothelin Receptor
- 体内研究：
Darusentan (30 mg/kg per day orally for weeks 3 and 4) reverses aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg per min subcutaneously for 2 and 4 weeks) in male Sprague Dawley rats. Animal Model: Twenty-four (eight per group) male Sprague Dawley rats weighing 175±200 g Dosage: 30 mg/kg Administration: Administered orally in rat food for weeks 3 and 4 Result: Reversed aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg).
- 参考文献：
1. Frank Enseleit, et al. Darusentan, a selective endothelin A receptor antagonist, for the oral treatment of resistant hypertension. Ther Adv Cardiovasc Dis. 2010 Aug;4(4):231-40. 2. Liang F, et al. Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries. Can J Physiol Pharmacol. 2010 Aug;88(8):840-9. 3. H H Dao, et al. Norepinephrine-induced aortic hyperplasia and extracellular matrix deposition are endothelin-dependent. J Hypertens. 2001 Nov;19(11):1965-73.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.437 ml 12.183 ml 24.365 ml 5 mM 0.487 ml 2.437 ml 4.873 ml 10 mM 0.244 ml 1.218 ml 2.437 ml 50 mM 0.049 ml 0.244 ml 0.487 ml
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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 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
