SAR502250-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESAR502250Cat.No.:HY-137472CASNo.:503860-57-9分?式:C??H??FN?O?分?量:367.38作?靶點:GSK-3作?通路:PI3K/Akt/mTOR;StemCell/Wnt儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(272.20mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7220mL13.6099mL27.2198mL5mM0.5444mL2.7220mL5.4440mL10mM0.2722mL1.3610mL2.7220mL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%salineSolubility:≥2.5mg/mL(6.80mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.80mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性SAR502250?種有效的，選擇性的，ATP競爭性，具有?服活性和可透過?腦屏障的GSK3抑制劑，對?GSK-3β的IC50值為12nM。SAR502250顯?出抗抑郁樣活性。SAR502250可?于研究阿爾茨海默癥(AD)。IC50&TargethGSK-3β12nM(IC50)體外研究SAR502250(0.01-1μM;36h)attenuatestheAβ25-35-inducedcelldeathinratembryonichippocampalneurons[2].體內(nèi)研究SAR502250(1-100mg/kg;asinglep.o,)attenuatestauhyperphosphorylationinthecortexandspinalcordoftransgenicmiceexpressingP301Ltau[2].SAR502250(10-30mg/kg;p.o.oncedailyfor7weeks)improvesthecognitivedeficitintransgenicAPP(SW)/Tau(VLW)miceafterinfusionofAβ25-35[2].SAR502250(10-30?mg/kg;asinglep.o.)significantlyincreasesthepercentageoflever-pressesintheinter-responsetime(IRT)bin(49-96?s),withasignificantaugmentationofthepercentageofreinforcedresponses[2].SAR502250(30?mg/kg;i.p.oncedailyfor28d)ameliorateschronicstress-induceddegradationofthephysicalstateofthemicecoat[2].SAR502250(10-60mg/kg;asinglep.o.)decreaseshyperactivityproducedbypsychostimulantsinmice[2].AnimalModel:FemaleP301Lhumantautransgenicmice(three-month-old;32g)[2]Dosage:1,3,10,30,100mg/kgAdministration:Asinglep.o.Result:Attenuateddose-dependentlytauphosphorylationinthecortexandspinalcord,withED50sof12.5and11.5?mg/kg,respectively.REFERENCES[1].FukunagaK,et,al.2-(2-Phenylmorpholin-4-yl)pyrimidin-4(3H)-ones;anewclassofpotent,selectiveandorallyactiveglycogensynthasekinase-3βinhibitors.BioorgMedChemLett.2013Dec15;23(24):6933-7.[2].GriebelG,et,al.TheselectiveGSK3inhibitor,SAR502250,displaysneuroprotectiveactivityandattenuatesbehavioralimpairmentsinmodelsofneuropsychiatricsymptomsofAlzheimer'sdiseaseinrodents.SciRep.2019Dec2;9(1):18045.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedfo