BMS-986020-AM152-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBMS-986020Cat.No.:HY-100619CASNo.:1257213-50-5Synonyms:AM152分⼦式:C₂₉H₂₆N₂O₅分⼦量:482.53作⽤靶点:LPLReceptor作⽤通路:GPCR/GProtein储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(518.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0724mL10.3621mL20.7241mL5mM0.4145mL2.0724mL4.1448mL10mM0.2072mL1.0362mL2.0724mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.31mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.31mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BMS-986020(AM152)⾼亲和⼒溶⾎磷脂酸受体1(LPA1)拮抗剂。BMS-986020抑制胆汁酸和磷脂转运蛋⽩，抑制BSEP，MRP4和MDR3，IC50值分别为4.8μM，6.2μM和7.5μM。BMS-986020有潜⼒⽤于特发性肺纤维化(IPF)的研究。IC50&TargetIC50:4.8µM(BSEP);6.2µM(MRP4);7.5µM(MDR3)[2]体外研究BMS-986020(0.1-10nM;pre-incubated)concentration-dependentdisplacementof[18F]BMT-083133bindingisobservedinLPA1+cellsandlungsections.At0.1nM,thepercentdisplacementinhealthymice,bleomycinmice,andIPFlungsis18%,24%,and31%,respectively.At10nM,thepercentdisplacementis73%,76%,and64%,respectively.[18F]BMT-083133,aradioligandtargetingLPA1isdevelopedasatranslationalresearchtoolforassessmentoflungLPA1engagementofBMS-986020usinginvitroautoradiography(ARG)[4].户使⽤本产品发表的科研⽂献•SciAdv.2021Sep17;7(38):eabb5933.•CellRep.2019Nov12;29(7):1832-1847.e8.•Carcinogenesis.2020Dec28;bgaa143.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KiharaY,etal.Lysophospholipidreceptorsindrugdiscovery.ExpCellRes.2015May1;333(2):171-7.[2].GlennRosen,etal.LPA1antagonistsBMS-986020andBMS-986234foridiopathicpulmonaryfibrosis:Preclinicalevaluationofhepatobiliaryhomeostasis.EuropeanRespiratoryJournal.[3].PalmerSM,etal.Randomized,Double-Blind,Placebo-Controlled,Phase2TrialofBMS-986020,aLysophosphatidicAcidReceptorAntagonistfortheTreatmentofIdiopathicPulmonaryFibrosis.Chest.2018Nov;154(5):1061-1069.[4].AdriennePena,etal.Autoradiographicevaluationof[18F]BMT-083133,alysophosphatidicacidreceptor1(LPA1)radioligand.Thejornalofnuclearmedicine.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl