MSDC-0160-Mitoglitazone-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMSDC0160Cat.No.:HY-100550CASNo.:146062-49-9Synonyms:Mitoglitazone;CAY10415分⼦式:C₁₉H₁₈N₂O₄S分⼦量:370.42作⽤靶点:InsulinReceptor;MitochondrialMetabolism作⽤通路:ProteinTyrosineKinase/RTK;MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:33.33mg/mL(89.98mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6996mL13.4982mL26.9964mL5mM0.5399mL2.6996mL5.3993mL10mM0.2700mL1.3498mL2.6996mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.75mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.75mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.75mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性MSDC0160(Mitoglitazone)调节噻唑烷⼆酮的线粒体靶标(mTOT)的胰岛素增敏剂，也线粒体丙酮酸载体(MPC)的调节剂。MSDC0160⼀种噻唑烷⼆酮(TZD)，具有抗糖尿病和神经保护活性作⽤。MSDC0160具有⽤于阿尔茨海默⽒病的潜⼒。体外研究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.体内研究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—您⾝边的抑制剂⼤师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