Darusentan

SKU: orb1220947

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.

Key Properties

• CAS Number: 171714-84-4
• MW: 410.43
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₂N₂O₆
• SMILES: COc1cc(OC)nc(O[C@H](C(O)=O)C(OC)(c2ccccc2)c2ccccc2)n1
• Target: Endogenous Metabolite
• Solubility: DMSO:125 mg/mL (304.57 mM);Water:Insoluble

Bioactivity

• 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. 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).
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• 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 ( 0.001-1 μM) inhibits ET-1-induced signaling in cultured RAVSMs.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Lu-135252

Quick Database Links

Gene Symbol

Endogenous Metabolite