CTPI-2-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesCTPI-2Cat.No.:HY-123986CASNo.:68003-38-3分?式:C??H?ClN?O?S分?量:356.74作?靶點(diǎn):MitochondrialMetabolism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(shí)驗(yàn)DMSO:125mg/mL(350.40mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8032mL14.0158mL28.0316mL5mM0.5606mL2.8032mL5.6063mL10mM0.2803mL1.4016mL2.8032mL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(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)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(shí)驗(yàn)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(shí)驗(yàn)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%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.08mg/mL(5.83mM);Clearsolution此?案可獲得≥2.08mg/mL(5.83mM，飽和度未知)的澄溶液。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2.體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。請依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.83mM);Clearsolution1/3此?案可獲得≥2.08mg/mL(5.83mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.08mg/mL(5.83mM);Clearsolution此?案可獲得≥2.08mg/mL(5.83mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性CTPI-2第三代特異性線粒體檸檬酸鹽載體SLC25A1抑制劑，KD為3.5μM。CTPI-2抑制糖酵解、PPARγ及其下游靶點(diǎn)葡萄糖轉(zhuǎn)運(yùn)蛋?GLUT4。CTPI-2阻斷?精性脂性肝炎逆轉(zhuǎn)脂變性的顯著改變，防?演變?yōu)橹愿窝?，減少肝臟和脂組織中炎性巨噬細(xì)胞的浸潤，并顯著減輕由?脂飲?引起的肥胖。具有抗腫瘤活性。IC50&TargetKD:3.5μM(SLC25A1)[1]體內(nèi)研究CTPI-2isauniqueregulatorofglycolysisthatlimitsthemetabolicplasticityofcancerstemcells(CSCs).CTPI-2(26?mg/kg;i.p.)inhibitstumorgrowthininvivomodelsofnon-smallcelllungcancer(NSCLC)[1].CTPI-2(50mg/kg;i.p.;alternatedaysfor12weeks)completelyavertsweightgaininthepreventionstudyandleadstosignificantweightlossinthereversionstudy[2].CTPI-2preventssteatohepatitisandnormalizesglucosetolerance.CTPI-2lowersthelevelsofcirculatingIL-6whileincreasinganti-inflammatoryIL-4andIL-10andalsoreducedthemonocytechemoattractantprotein-1andmonokine-inducedbyinterferon-γthatattractneutrophilsandmonocytes.CTPI-2regulatesthecitratepool,thelipogenicandthegluconeogenicpathways[2].AnimalModel:C57BL/6Jmice(HFD-fedmice)[2]Dosage:50mg/kgAdministration:Alternatedaysviatheintraperitonealroutefor12weeksResult:Completelyavertedweightgaininthepreventionstudyandledtosignificantweightlossinthereversionstudy.REFERENCES[1].TanM,etal.Inhibitionofthemitochondrialcitratecarrier,Slc25a1,revertssteatosis,glucoseintolerance,andinflammationinpreclinicalmodelsofNAFLD/NASH.CellDeathDiffer.2020;27(7):2143-2157.[2].FernandezHR,etal.Themitochondrialcitratecarrier,SLC25A1,drivesstemnessandtherapyresistanceinnon-smallcelllungcancer.CellDeathDiffer.2018;25(7):1239-1258.McePdfHeight2