BI-749327-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBI-749327Cat.No.:HY-111925CASNo.:2361241-23-6分⼦式:C₂₃H₂₁F₃N₄O₂分⼦量:442.43作⽤靶点:TRPChannel作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:31.25mg/mL(70.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2602mL11.3012mL22.6024mL5mM0.4520mL2.2602mL4.5205mL10mM0.2260mL1.1301mL2.2602mL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。-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%salineSolubility:≥2.08mg/mL(4.70mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.70mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.70mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BI-749327⼀种⾼效、⾼选择性、有⼝服⽣物活性的TRPC6拮抗剂，对⼩⿏、⼈、豚⿏TRPC6作⽤的IC50值分别为13nM、19nM和15nM。BI-749327对⼩⿏TRPC6的选择性TRPC3的85倍，TRPC7的42倍[1]。IC50&TargetIC50:13nM(mouseTRPC6),19nM(humanTRPC6),15nM(guineapigTRPC6)[1]体外研究BI-749327suppressesNFATactivationinHEK293Tcellsexpressingwild-typeorgain-of-functionTRPC6mutantsandblocksassociatedsignalingandexpressionofprohypertrophicgenesinisolatedmyocytes[1].体内研究BI-749327(30mg/kg/day;i.g.)improvesleftheartfunction,reducesvolume/massratio,andbluntsexpressionofprofibroticgenesandinterstitialfibrosisinmicesubjectedtosustainedpressureoverload[1].BI-749327dosedependentlyreducesrenalfibrosisandassociatedgeneexpressioninmicewithunilateralureteralobstruction[1].BI-749327haslongterminalhalf-life(t1/28.5-13.5hours)formice(3-30mg/kg;p.o.)[1].AnimalModel:C57BL/6Jmice[1]Dosage:30mg/kg/dayAdministration:OralgavageResult:Improvedleftheartfunction,reducedvolume/massratio,andbluntedexpressionofprofibroticgenesandinterstitialfibrosisinmicesubjectedtosustainedpressureoverload.AnimalModel:CD-1mice[1]Dosage:3mg/kg,10mg/kg,30mg/kgAdministration:OraladministrationResult:t1/28.5-13.5hours户使⽤本产品发表的科研⽂献•BiochimBiophysActaMolBasisDis.2022Jul23;166505.•AmJPhysiolLungCellMolPhysiol.2021Oct27.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•AmJPhysiolCellPhysiol.2022Aug15.•SciRep.2022Feb22;12(1):3038.•Biomedicines.2022,10(7),1574.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LinBL,etal.InvivoselectiveinhibitionofTRPC6byantagonistBI749327amelioratesfibrosisanddysfunctionincardiacandrenaldisease.ProcNatlAcadSciUSA.2019May14;116(20):10156-10161.McePdfHeightCaution:Producthasnotbeenfullyvalidated