Darusentan (Synonyms: HMR 4005, Lu 135252) |
| Catalog No.GC35811 |
Darusentan (Lu-135252) es un antagonista selectivo del receptor del receptor de endotelina A (ET-A), que se une con una Ki de 1,4 nM al receptor ET-A y una Ki de 184 nM al receptor ET-B, respectivamente con un 100 -veces selectividad para los receptores ETA en lugar de 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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