Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBMS-986020Cat.No.:HY-100619CASNo.:1257213-50-5Synonyms:AM152分?式:C??H??N?O?分?量:482.53作?靶點(diǎn):LPLReceptor作?通路:GPCR/GProtein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:250mg/mL(518.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0724mL10.3621mL20.7241mL5mM0.4145mL2.0724mL4.1448mL10mM0.2072mL1.0362mL2.0724mL請根據(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?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.31mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.31mM);ClearsolutionBIOLOGICALACTIVITY?物活性BMS-986020(AM152)?親和?溶?磷脂酸受體1(LPA1)拮抗劑。BMS-986020抑制膽汁酸和磷脂轉(zhuǎn)運(yùn)蛋?，抑制BSEP，MRP4和MDR3，IC50值分別為4.8μM，6.2μM和7.5μM。BMS-986020有潛??于特發(fā)性肺纖維化(IPF)的研究。IC50&TargetIC50:4.8μM(BSEP);6.2μM(MRP4);7.5μM(MDR3)[2]體外研究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].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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