| 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： |
-80℃（运输条件：冰袋低温运输） |
| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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