Darusentan (Synonyms: HMR 4005, Lu 135252) |
| رقم الكتالوجGC35811 |
Darusentan (Lu-135252) هو أحد مضادات مستقبلات البطانة A (ET-A) الانتقائية ، والتي ترتبط بـ Ki البالغ 1.4 نانومتر إلى مستقبل ET-A و Ki من 184 نانومتر إلى مستقبل ET-B ، على التوالي مع 100 انتقائية مضاعفة لـ ETA بدلاً من مستقبلات ETB
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Cas No.: 171714-84-4
Sample solution is provided at 25 µL, 10mM.
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Darusentan is a selective endothelin A (ETA) receptor antagonist. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki=13 nM[1].
[1]. 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.
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