UNC2881-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEUNC2881Cat.No.:HY-15798CASNo.:1493764-08-1分?式:C??H??N?O?分?量:463.58作?靶點(diǎn):TAMReceptor作?通路:ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥44mg/mL(94.91mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1571mL10.7856mL21.5713mL5mM0.4314mL2.1571mL4.3142mL10mM0.2157mL1.0786mL2.1571mL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。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(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，澄的儲備液可以根據(jù)儲存條件，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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.39mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.39mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.39mM);ClearsolutionBIOLOGICALACTIVITY?物活性UNC2881?種?服有效、特異性的Mer激酶抑制劑，可抑制穩(wěn)定狀態(tài)的Mer激酶磷酸化，IC50為22nM。UNC2881對Axl和Tyro也有抑制作?，IC50分別為360nM和250nM。UNC2881可有效抑制膠原誘導(dǎo)的??板聚集，可?于?栓病理研究。IC50&TargetIC50:4.3nM(Mer),360nM(Axl),250nM(Tyro)[1]體外研究UNC2881(compound23)(0-1000nM;1h)blockligand-stimulatedactivationofachimericEGFR-MerTK.UNC2881alsoinhibitsendogenousMertyrosinekinaseactivationinacutelymphoblasticleukemiacells[1].UNC2881(3μM;1h)suppressesplateletaggregationbygreaterthan25%inhumanplatelet-richplasmainresponsetostimulationwithfibrillartypeIequinecollagen[1].WesternBlotAnalysis[1]CellLine:32DcellsConcentration:0,10,30,100,300,1000nMIncubationTime:1hour;priortostimulationwith100ng/mLEGFligandfor15minResult:Reducedthephospho-tyrosinelevelinadose-dependentmanner.體內(nèi)研究UNC2881(3mg/kg;p.o.;singledose)hashighsystemicclearance(94.5mL/min/kg)and14%oralbioavailability,displaysterminalhalf-lifeof0.80h[1].UNC2881(3mg/kg;i.v.;injectedwithVSVondays-3,-2,-1,and0)limitsMertksignaling,andpromotestheantiviralimmuneresponse,reducingtheviralreplicationofvesicularstomatitisvirus(VSV)ininfectedmice[2].PharmacokineticsofUNC2881inmice[1]RouteDose(mg/kg)T1/2(h)Tmax(h)Cmax(ng/mL)AUClast(ng·h/mL)CLobs(mL/min)Vss(L/kg)F(%)IV30.8260952794.51.65PO30.3090.071.714AnimalModel:C57BL/6mice(7-10weeksold)[2]Dosage:3mg/kgAdministration:Intravenousinjection;infectedwith2×108PFUvesicularstomatitisvirus(VSV)(i.v.)ondays-3,-2,-1,and02/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:ReducedVSVreplicationinspleen,liver,kidney,lung.REFERENCES[1].TomAdomati,etal.DeadCellsInduceInnateAnergyViaMertkafterAcuteViralInfection.CellReports.2020.30(11):3671-3681.[2].ZhangW,etal.DiscoveryofMerspecifictyrosinekinaseinhibitorsforthetreatmentandpreventionofthrombosis.JMedChem.2013Dec12;56(23):9693-700.McePdfHeightCaution:Producthasnotbeenfullyva