Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesMID-1Cat.No.:HY-115461CASNo.:312608-54-1分?式:C??H??N?O?S分?量:293.3作?靶點:InsulinReceptor作?通路:ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:31.25mg/mL(106.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.4095mL17.0474mL34.0948mL5mM0.6819mL3.4095mL6.8190mL10mM0.3409mL1.7047mL3.4095mL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，并請注意儲備液的保存?式和期限。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%DMSO40%PEG3005%Tween-8045%salineSolubility:2.08mg/mL(7.09mM);Suspendedsolution;Needultrasonic此?案可獲得2.08mg/mL(7.09mM)的均勻懸濁液，懸濁液可?于?服和腹腔注射。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。1/3BIOLOGICALACTIVITY?物活性MID-1?種MG53-IRS-1(Mitsugumin53-胰島素受體底物1)相互作?的抑制劑。MID-1破壞了MG53與IRS-1的分?締合，并消除了MG53誘導的IRS-1泛素化和?骼肌降解，從?導致IRS-1表達?平升?，胰島素信號傳導和葡萄糖攝取增加。體外研究MID-1(5μM;24h)increasestheIRS-1expressionlevelinskeletalmusclebydisruptingtheMG53-IRS-1interaction[1].MID-1(10μM;12h)reducestheluciferaseactivityinHEK293celllineexpressingNLUC-IRS-1andCLUC-C14A[1].MID-1(1-20μM;12h)disruptstheMG53-IRS-1interactionbutnotMG53-FAKinteractioninHEK293cells[1].MID-1(0.1-10μM;4-24h)abolishesMG53-inducedIRS-1ubiquitinationanddegradationinHEK293cells[1].MID-1(5-10μM;24h)increasesinsulinsignalingandinsulin-elicitedglucoseuptakeinC2C12myotubes[1].MID-1(5-10μM;24h)enhancesskeletalmyogenesis[1].WesternBlotAnalysis[1]CellLine:C2C12myotubesConcentration:5μMIncubationTime:24hResult:IncreasedtheIRS-1proteinlevel.體內(nèi)研究MID-1doesnothavegoodpharmacokineticsinvivo[1].REFERENCES[1].LeeH,et,al.MG53-IRS-1(Mitsugumin53-InsulinReceptorSubstrate-1)InteractionDisruptorSensitizesInsulinSignalinginSkeletalMuscle.JBiolChem.2016Dec23;291(52):26627-26635.McePdfHeight2/3MedChemExpress(MCE)只為有資質(zhì)的科研機構、醫(yī)藥企業(yè)基于科學研