Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMSDC0160Cat.No.:HY-100550CASNo.:146062-49-9Synonyms:Mitoglitazone;CAY10415分?式:C??H??N?O?S分?量:370.42作?靶點:InsulinReceptor;MitochondrialMetabolism作?通路:ProteinTyrosineKinase/RTK;MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據體外實驗DMSO:33.33mg/mL(89.98mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6996mL13.4982mL26.9964mL5mM0.5399mL2.6996mL5.3993mL10mM0.2700mL1.3498mL2.6996mL請根據產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?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據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儲存條件，適當保存；體內實驗的?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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(6.75mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.75mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.75mM);ClearsolutionBIOLOGICALACTIVITY?物活性MSDC0160(Mitoglitazone)調節(jié)噻唑烷?酮的線粒體靶標(mTOT)的胰島素增敏劑，也線粒體丙酮酸載體(MPC)的調節(jié)劑。MSDC0160?種噻唑烷?酮(TZD)，具有抗糖尿病和神經保護活性作?。MSDC0160具有?于阿爾茨海默?病的潛?。體外研究MSDC0160(Mitoglitazone;1-50μM;for24hours)significantlydecreasesphosphorylationofmTORat20and50μM[1].MSDC0160actsasinsulinsensitizerswithoutactivatingPPARγ[1].MSDC0160(10μM;pretreatment1hour)preventstheMPP+(10μM)-inducedlossofbothtyrosinehydroxylase(TH)-immunoreactivedifferentiatedLundhumanmesencephalic(LUHMES)cells[1].MSDC0160(10or100μM)preventsthelossofGFP-fluorescentdopaminergicneuronsinducedbyMPP+(0.75mM)innematodes[1].MSDC0160(10-20μM)inconbinationwithIGF-1preventsthelossofinsulincontentandmaintainsinsulinsecretion[1].MSDC0160(1-50μM)treatmentmaintainshumanβ-cellphenotype[2].WesternBlotAnalysis[1]CellLine:HumanisletsConcentration:1,10,20,50μMIncubationTime:For24hoursResult:SignificantlydecreasedPhosphorylationofmTORat20and50μM.體內研究MSDC0160(Mitoglitazone;30mg/kg;oralgavage;daily;for7days)improveslocomotorbehavior,increasessurvivalofnigraldopaminergicneurons,boostsstriataldopaminelevels,andreducesneuroinflammationin1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine(MPTP)-treatedmice[2].AnimalModel:Ten-to12-week-oldmaleC57BL/6Jmiceweighing24to28g[2]Dosage:30mg/kgAdministration:Oralgavage;daily;for7daysResult:Improvedlocomotorbehavior,increasedsurvivalofnigraldopaminergicneurons,2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEboostedstriataldopaminelevels,andreducedneuroinflammation.REFERENCES[1].RohatgiN,etal.Novelinsulinsensitizermodulatesnutrientsensingpathwaysandmaintainsβ-cellphenotypeinhumanislets.PLoSOne.2013May1;8(5):e62012.[2].GhoshA,etal.Mitochondrialpyruvatecarrierregulatesautophagy,inflammation,andneurodegenerationinexperimentalmodelsofParkinson'sdisease.SciTranslMed.2016Dec7;8(368):368ra174.McePdfHeightCaution:Producthasnotbeenfull