Darusentan

Research use only, not for human use.

Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries.

Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries.(In Vitro):Darusentan ((S)-Darusentan) competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki=13 nM. In isolated endothelium-denuded rat aortic rings, Darusentan inhibits endothelin-induced vascular contractility with a pA2=8.1±0.14. Darusentan ( 0.001-1μM) inhibits ET-1-induced signaling in cultured RAVSMs.(In Vivo):Darusentan (30 mg/kg per day orally for weeks 3 and 4) reverses aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg per min subcutaneously for 2 and 4 weeks) in male Sprague Dawley rats.

Darusentan ((S)-Darusentan) competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki=13 nM. In isolated endothelium-denuded rat aortic rings, Darusentan inhibits endothelin-induced vascular contractility with a pA2=8.1±0.14. Darusentan ( 0.001-1μM) inhibits ET-1-induced signaling in cultured RAVSMs.

Darusentan (30 mg/kg per day orally for weeks 3 and 4) reverses aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg per min subcutaneously for 2 and 4 weeks) in male Sprague Dawley rats. Animal Model:Twenty-four (eight per group) male Sprague Dawley rats weighing 175±200 g Dosage:30 mg/kg Administration:Administered orally in rat food for weeks 3 and 4 Result:Reversed aortic alterations produced by infusion of Norepinephrine (2.5 μg/kg).

Lu-135252

Proteasome/Ubiquitin

Endogenous Metabolite

Endothelin A receptor

Metabolic Disease

Arrhythmias; Diabetic angiopathies; Diabetic nephropathies; Heart failure; Ischaemic heart disorders

171714-84-4

410.43

C22H22N2O6

>98% (HPLC)

DMSO:125 mg/mL (304.57 mM);Water:Insoluble

COc1cc(OC)nc(O[C@H](C(O)=O)C(OC)(c2ccccc2)c2ccccc2)n1

(S)-2-((46-Dimethoxy-2-pyrimidinyl)oxy)-3-methoxy-33-diphenylpropionic acid

(-20℃)

With Ice Pack

≥ 2 years