Formulation: A solid
Formal Name: αS-[(4,6-dimethoxy-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-benzenepropanoic acid
Purity: ≥98%
Formula Markup: C22H22N2O6
Formula Weight: 410,4
Shelf life (days): 1460
CAS Number: 171714-84-4
Notes: Darusentan is an endothelin type A (ETA) receptor antagonist (Ki = 13 nM in rat aortic vascular smooth muscle cells).{64593} It inhibits contractions induced by human endothelin-1 (ET-1; Item No. 24127) in isolated rat aortic rings and mesenteric microvessels with pA2 values of 8.1 and 7.97, respectively. Darusentan (50 mg/kg) decreases systolic blood pressure in DOCA-salt hypertensive rats, as well as reduces mean arterial pressure (MAP) and left ventricular developed pressure (LVDP) in normotensive pigs when administered at doses of 1 and 5 mg/kg.{64594,64595} It reduces myocardial infarct size as a percentage of the area at risk in a porcine model of ischemia-reperfusion injury induced by ligation of the left anterior descending (LAD) coronary artery.{64595}
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