Taminadenant-NIR178-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETaminadenantCat.No.:HY-109139CASNo.:1337962-47-6Synonyms:NIR178;PBF509分?式:C??H?BrN?分?量:306.12作?靶點:AdenosineReceptor作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(408.34mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.2667mL16.3335mL32.6669mL5mM0.6533mL3.2667mL6.5334mL10mM0.3267mL1.6333mL3.2667mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?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：(為保證實驗結(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)實驗的?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:≥2.08mg/mL(6.79mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.79mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.79mM);ClearsolutionBIOLOGICALACTIVITY?物活性Taminadenant(NIR178;PBF509)?種?效且具有?服活性的腺苷A2A受體(adenosineA2Areceptor)拮抗劑。Taminadenant可拮抗A2AR激動劑介導(dǎo)的cAMP積累和阻抗反應(yīng)，KB值分別為72.8nM和8.2nM。Taminadenant能逆轉(zhuǎn)運動障礙??模型的運動障礙，包括僵硬、震顫和偏側(cè)震顫?痹。與Spartalizumab(HY-P9972)聯(lián)合使?時，Taminadenant還能夠抑制腫瘤?長。Taminadenant能重新激活抗腫瘤免疫反應(yīng)。IC50&TargetAdenosinereceptor[1]體外研究Taminadenant(PBF509)doesnotshowanyagonistefficacyinHEKcellspermanentlyexpressingthehumanA2ARSNAP,butcompletelyantagonizestheagonist-mediatedcAMPaccumulationinA2ARSNAPexpressingHEKcellswithanIC50of72.8±17.4nM[1].體內(nèi)研究Taminadenant(PBF509)(0.3,3,7.5,10,or30mg/kg;p.o.;singledosage)attenuatesthecatalepticeffectsofHaloperidol,attenuatespilocarpine-inducedtremulousjawmovement,enhancestheeffectsofL-DOPA,showsarobustantiparkinsonianactivityanddisplaysantidyskineticefficacy[1].AnimalModel:Sprague-Dawleyrats(240-250g;inducedcatalepsybys.c.with1mg/kgHaloperidol(HY-14538))[1]Dosage:3,10,or30mg/kgAdministration:p.o.;singledosageResult:Dose-dependentlyattenuatedthecatalepticeffectsofHaloperidolwhenadministered1hafterHaloperidolinjection.AnimalModel:Sprague-Dawleyrats(240-250g;inducedtremulousjawmovementbys.c.with1mg/kgPilocarpine(HY-B0726A))[1]Dosage:0.3,3,or7.5mg/kgAdministration:p.o.;singledosageResult:Dose-dependentlyattenuatedpilocarpine-inducedtremulousjawmovement,beingeffectiveatthelowestdosetested.AnimalModel:Sprague-Dawleyrats(240-250g;inducedhemiparkinsonianbyunilateralinjectionof6-2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEOHDA(HY-B1081)inthemedialforebrainbundle)[1]Dosage:0.3and3mg/kgAdministration:p.o.;singledosageResult:EnhancedtheeffectsofL-DOPAwithaminimumefficaciousdose(MED)of3mg/kgp.o..AnimalModel:Sprague-Dawleyrats(240-250g;induceddyskinesiasbyi.p.4mg/kgL-DOPA(HY-N0304)for14daysandi.p.15mg/kgBenserazidehydrochloride(HY-B0404A))[1]Dosage:0.3or3mg/kgAdministration:p.o.;singledosageResult:Showedarobustantiparkinsonianactivityanddisplayedantidyskineticefficacy.REFERENCES[1].Nú?ezF,etal.PBF509,anAdenosineA2AReceptorAntagonistWithEfficacyinRodentModelsofMovementDisorders.FrontPharmacol.2018Oct19;9:1200.[2].ChiapporiAA,etal.PhaseIStudyofTaminadenant(PBF509/NIR178),anAdenosine2AReceptorAntagonist,withorwithoutSpartalizumab(PDR001),inPatientswithAdvancedNon-SmallCellLungCancer.ClinCancerRes.2022Jun1;28(11):2313-2320.McePdfHeightCaution:P