CMS-121-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECMS-121Cat.No.:HY-135981CASNo.:1353224-53-9分?式:C??H??NO?分?量:321.37作?靶點:Acetyl-CoACarboxylase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(155.58mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1117mL15.5584mL31.1168mL5mM0.6223mL3.1117mL6.2234mL10mM0.3112mL1.5558mL3.1117mL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?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：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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:≥2.08mg/mL(6.47mM);Clearsolution1/2MasterofBioactiveMolecules—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:≥2.08mg/mL(6.47mM);ClearsolutionBIOLOGICALACTIVITY?物活性CMS-121?種喹諾酮衍?物，也?種?服活性的?酰輔酶A羧化酶1(acetyl-CoAcarboxylase1,ACC1)抑制劑。CMS-121分別以EC50值為7nM和200nM來保護HT22細胞免受缺?和氧化損傷。CMS-121具有強?的神經(jīng)保護，抗炎，抗氧化和腎保護作?。IC50&TargetAcetyl-CoAcarboxylase1(ACC1)[1]體外研究CMS-121(1μM;4hours;HT22cells)treatmentincreasesthephosphorylationofACC1atserine79.CMS-121canincreaseacetyl-CoAincells[1].WesternBlotAnalysis[1]CellLine:HT22cellsConcentration:1μMIncubationTime:4hoursResult:IncreasesthephosphorylationofACC1atserine79.體內(nèi)研究CMS-121(~20mg/kg;oraladministration;daily;for4months;femaleSAMP8mice)treatmentreducescognitivedeclineaswellasmetabolicandtranscriptionalmarkersofaginginthebrainwhenadministeredtorapidlyagingSAMP8mice.CMS-121preservesmitochondrialhomeostasisbyregulatingacetyl-coenzymeA(acetyl-CoA)metabolism[1].AnimalModel:FemaleSAMP8mice(9monthsold)[1]Dosage:~20mg/kg/dayAdministration:Oraladministration;daily;for4monthsResult:Reducedcognitivedeclineaswellasmetabolicandtranscriptionalmarkersofaginginthebrain.REFERENCES[1].CurraisA,etal.Elevatingacetyl-CoAlevelsreducesaspectsofbrainaging.Elife.2019Nov19;8.pii:e47866.[2].ChirutaC,etal.Chemicalmodificationofthemultitargetneuroprotectivecompoundfisetin.JMedChem.2012Jan12;55(1):378-89.[3].PriorM,etal.Backtothefuturewithphenotypicscreening.ACSChemNeurosci.2014Jul16;5(7):503-13.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplicati