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Darusentan

CAT: 0013-GTR19158148-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19158148-01Size:200 mg
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Description
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.
CAS Number
171714-84-4
Product Name Alternative
Lu-135252
Purity
>98% (HPLC)
Solubility
DMSO:125 mg/mL (304.57 mM) ; Water:Insoluble
Smiles
COc1cc (OC) nc (O[C@H] (C (O) =O) C (OC) (c2ccccc2) c2ccccc2) n1
Molecular Formula
C22H22N2O6
Molecular Weight
410.43
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
(S) -2- ((46-Dimethoxy-2-pyrimidinyl) oxy) -3-methoxy-33-diphenylpropionic acid

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