Darusentan 是一种选择性内皮素 A (endothelin A; ETA) 受体拮抗剂。Darusentan 在大鼠主动脉血管平滑肌细胞 (RAVSMs) 膜中竞争结合放射性标记的内皮素,Ki 为 13 nM。
CAS:171714-84-4
分子式:C22H22N2O6
分子量:410.42
纯度:98%
存储:Store at -20°C
Background:
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.