Darusentan (Synonyms: HMR 4005, Lu 135252) |
| カタログ番号GC35811 |
ダルセンタン (Lu-135252) は、選択的エンドセリン受容体 A (ET-A) 受容体アンタゴニストであり、ET-A 受容体には 1.4 nM の Ki で、ET-B 受容体には 184 nM の Ki で、それぞれ 100 で結合します。 -ETB 受容体よりも ETA に対する選択性が倍増します。
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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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