R-Verapamil-Dexverapamil-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE(R)-VerapamilCat.No.:HY-Z15823CASNo.:38321-02-7Synonyms:Dexverapamil分⼦式:C₂₇H₃₈N₂O₄分⼦量:454.6作⽤靶点:CalciumChannel;PotassiumChannel;SomatostatinReceptor;Arrestin;Apoptosis;P-glycoprotein作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling;GPCR/GProtein;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性(R)-Verapamil(Dexverapamil)⼀种⼝服有效的Verapamil(HY-14275)的光学对映体。(R)-Verapamil对L型钙通道(Cav1.2)的亲和⼒较低(IC50>300μM)，对钠离⼦通道(sodiumchannel)的IC50为3.19μM。(R)-Verapamil具有SSTR2激动活性，其EC50为1.3μM。(R)-Verapamil在糖尿病⼩⿏模型中显著下调TXNIP蛋⽩表达，并显著抑制β细胞凋亡(apoptosis)，有效控制⾎糖。(R)-Verapamil可作为P-糖蛋⽩(P-gp)功能的PET⽰踪剂。REFERENCES[1].ChenYS,etal.EvaluatingtheantidiabeticeffectsofR-verapamilintype1andtype2diabetesmellitusmousemodels.PLoSOne.2021Aug6;16(8):e0255405.[2].BusseD,etal.Cardiovasculareffectsof(R)-and(S)-verapamilandracemicverapamilinhumans:aplacebo-controlledstudy.EurJClinPharmacol.2006Aug;62(8):613-9.[3].LuurtsemaG,etal.(R)-and(S)-[11C]verapamilasPET-tracersformeasuringP-glycoproteinfunction:invitroandinvivoevaluation.NuclMedBiol.2003Oct;30(7):747-51.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792ax:021