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[1]. 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[2].
Molecular Weight:
410.42
Purity:
98.67
CAS Number:
[171714-84-4]
Formula:
C22H22N2O6
Target:
Endothelin Receptor
Application Notes:
MCE Product type: Reference compound
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