Eprosartan-d6-SKF-108566J-free-base-d-sub-6-sub-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEEprosartan-d6Cat.No.:HY-117743S1Synonyms: SKF-108566Jfreebase-d6分子式: C₂₃H₁₈D₆N₂O₄S分子量: 430.55作用靶点: AngiotensinReceptor;Isotope-LabeledCompounds作用通路: GPCR/GProtein;Others储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Eprosartan-d6是氘代标记的Eprosartan(HY-117743)。Eprosartan(SKF-108566Jfreebase)是一种选择性，竞争性，非肽和具有口服活性的血管紧张素II受体(angiotensinIIreceptor)拮抗剂，可用作降压剂。Eprosartan结合血管紧张素II受体，在大鼠和人类肾上腺皮质膜中的IC50值分别为9.2nM和3.9nM。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].Eprosartan(SKF-108566J)inhibits[125I]AIIbindingtohumanlivermembranes(IC50of1.7nM)andtoratmesentericarterymembranes(IC50of1.5nM).Inrabbitaorticsmoothmusclecells,Eprosartancausedaconcentration-dependentinhibitionofAII-inducedincreasesinintracellularCa2+levels[2].体内研究Inconsciousnormotensiverats,i.v.administrationofEprosartan(0.01-0.3mg/kg)produceddose-dependentparallelshiftsintheAIIpressordose-responsecurve.AdministrationofEprosartan(3-10mg/kg)intraduodenallyorintragastricallytoconsciousnormotensiveratsresultedinadose-dependentinhibitionofthepressorresponsetoAII(250ng/kg,i.v.).At10mg/kg,i.d.,significantinhibitionofthepressorresponsetoAIIwasobservedfor3hr[2].REFERENCESRMEdwards,etal.PharmacologicalcharacterizationofthenonpeptideangiotensinIIreceptorantagonist,SK&F108566.JPharmacolExpTher.1992Jan;260(1):175-81.RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: