Description
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. 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.
Product information
CAS Number: 171714-84-4
Molecular Weight: 410.42
Formula: C22H22N2O6
Chemical Name: (2S)-2-[(4,6-dimethoxypyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid
Smiles: COC1C=C(N=C(N=1)O[C@H](C(O)=O)C(OC)(C1C=CC=CC=1)C1C=CC=CC=1)OC
InChiKey: FEJVSJIALLTFRP-LJQANCHMSA-N
InChi: InChI=1S/C22H22N2O6/c1-27-17-14-18(28-2)24-21(23-17)30-19(20(25)26)22(29-3,15-10-6-4-7-11-15)16-12-8-5-9-13-16/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 125 mg/mL (304.57 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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