Verapamil-racemic-Verapamil-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVerapamilCat.No.:HY-14275CASNo.:52-53-9Synonyms:(±)-Verapamil;CP-16533-1分⼦式:C₂₇H₃₈N₂O₄分⼦量:454.6作⽤靶点:CalciumChannel;P-glycoprotein;CytochromeP450作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling;MetabolicEnzyme/Protease储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:100mg/mL(219.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1997mL10.9987mL21.9974mL5mM0.4399mL2.1997mL4.3995mL10mM0.2200mL1.0999mL2.1997mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.50mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.50mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.50mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Verapamil((±)-Verapamil)⼀种钙通道(calciumchannel)阻滞剂，⼀种有效的⼝服活性的第⼀代P糖蛋⽩(P-gp)抑制剂。Verapamil能也抑制CYP3A4，并可⽤于⾼⾎压，⼼律不齐和⼼绞痛的研究。IC50&TargetCalciumchannel[1]Permeability-glycoprotein(P-gp)[1]CYP3A4[1]体外研究TheEverFluorFLVerapamil(EFV)uptakebyTR-iBRB2cellsisinhibitedbycationicdrugs,andinhibitsbyverapamilinaconcentration-dependentmannerwithanIC50of98.0μM[4].体内研究GivenorallyVerapamilisusefulfortheprophylaxisofatrioventricularreentrytachycardia,andalsoinmodulatingtheatrioventricularnodalresponseinatrialfibrillation[2].Voafemoralveinpriortoischemia.Verapamil(1mg/kg)significantlydecreasestheincidenceofventriculararrhythmiasincludingprematureventricularcontractions(PVC),ventriculartachycardia(VT)andventricularfibrillation(VF)for45-mincoronaryarteryocclusion.Totalarrhythmiascoresaresignificantlyincreasedwhentheheartissubjectedtoischemia.Verapamil(1mg/kg)significantlypreventstheenhancementoftotalarrhythmiascoresinducedbyischemia[5].户使⽤本产品发表的科研⽂献•CancerCell.2017Apr10;31(4):501-515.e8.•BioactMater.2021Apr21;6(11):4073-4082.•JPharmAnal.2020Apr;10(2):178-186.•BrJPharmacol.2021Jul3.•JMedChem.2021Mar11;64(5):2725-2738.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GowartyJL,etal.Verapamilasaculpritofpalbociclibtoxicity.JOncolPharmPract.2019Apr;25(3):743-746.[2].KriklerDM.Verapamilinarrhythmia.BrJClinPharmacol.1986;21Suppl2:183S-189S.[3].RehnqvistN,etal.Effectsofmetoprololvsverapamilinpatientswithstableanginapectoris.TheAnginaPrognosisStudyinStockholm(APSIS).EurHeartJ.1996Jan;17(1):76-81.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[4].KuboY,etal.Blood-to-RetinaTransportofFluorescence-LabeledVerapamilattheBlood-RetinalBarrier.PharmRes.2018Mar12;35(5):93.[5].ZhouP,etal.Anti-arrhythmiceffectofVerapamilisaccompaniedbypreservationofcx43proteininratheart.PLoSOne.2013Aug12;8(8):e71567.McePdfHeightCaution:Producthasnotb