BI-749327-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBI-749327Cat.No.:HY-111925CASNo.:2361241-23-6分?式:C??H??F?N?O?分?量:442.43作?靶點(diǎn):TRPChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:31.25mg/mL(70.63mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2602mL11.3012mL22.6024mL5mM0.4520mL2.2602mL4.5205mL10mM0.2260mL1.1301mL2.2602mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.70mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.70mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.70mM);ClearsolutionBIOLOGICALACTIVITY?物活性BI-749327?種?效、?選擇性、有?服?物活性的TRPC6拮抗劑，對(duì)??、?、豚?TRPC6作?的IC50值分別為13nM、19nM和15nM。BI-749327對(duì)??TRPC6的選擇性TRPC3的85倍，TRPC7的42倍[1]。IC50&TargetIC50:13nM(mouseTRPC6),19nM(humanTRPC6),15nM(guineapigTRPC6)[1]體外研究BI-749327suppressesNFATactivationinHEK293Tcellsexpressingwild-typeorgain-of-functionTRPC6mutantsandblocksassociatedsignalingandexpressionofprohypertrophicgenesinisolatedmyocytes[1].體內(nèi)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戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?BiochimBiophysActaMolBasisDis.2022Jul23;166505.?AmJPhysiolLungCellMolPhysiol.2021Oct27.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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