Perhexiline-maleate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPerhexilinemaleateCat.No.:HY-B1334ACASNo.:6724-53-4分⼦式:C₂₃H₃₉NO₄分⼦量:393.56作⽤靶点:MitochondrialMetabolism;Apoptosis作⽤通路:MetabolicEnzyme/Protease;Apoptosis储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验Ethanol:20mg/mL(50.82mM;Needultrasonic)DMSO:3.57mg/mL(9.07mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5409mL12.7045mL25.4091mL5mM0.5082mL2.5409mL5.0818mL10mM0.2541mL1.2705mL2.5409mL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(sealedstorage,awayfrommoisture)。-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%salineSolubility:≥0.5mg/mL(1.27mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥0.5mg/mL(1.27mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥0.5mg/mL(1.27mM);Clearsolution4.请依序添加每种溶剂：10%EtOH>>90%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(5.08mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Perhexilinemaleate⼀种具有⼝服活性的CPT1和CPT2抑制剂，可减少脂酸代谢。Perhexilinemaleate在肝细胞中诱导线粒体功能障碍和细胞凋亡(apoptosis)。Perhexilinemaleate可穿过⾎脑屏障(BBB)，并显⽰出抗肿瘤活性。Perhexilinemaleate可⽤于癌症和⼼绞痛等⼼⾎管疾病的研究。IC50&TargetIC50:77μM(RatheartCPT1),148μM(RatliverCPT1)[1]体外研究Perhexiline(5-25μM,2-6h)maleatereducescellviabilityinHepG2cells[2].Perhexiline(5-25μM,2-6h)maleatereducescellularATPcontentandLactatedehydrogenase(LDH)releaseinHepG2cells[2].Perhexiline(20μM,2h)maleateactivatescaspase3/7inHepG2cells[2].Perhexiline(5-25μM,4h)maleatecausesmitochondrialdysfunctioninHepG2cells[2].Perhexiline(5μM,48h)maleateselectivelyinducesmassiveapoptosisinCLLcells(highexpressionofCPT)[3].CellViabilityAssay[2]CellLine:HepG2cellsConcentration:5,10,15,25μMIncubationTime:2,4,6hResult:Inducedtime-andconcentration-dependentcytotoxicityinhepaticcells.WesternBlotAnalysis[2]CellLine:HepG2cellsConcentration:5,10,15,25μMIncubationTime:2hResult:ReducedBcl-2andMcl-1level,andincreasedBadlevel.体内研究Perhexiline(200mg/kg,p.o.,dailyfor8weeks)maleatereducesperipheralneuralfunctioninfemaleDArats[4].Perhexiline(80mg/kg,oralgavage,for3days)maleatedemonstratesanti-tumoractivityinglioblastomamousemodel[5].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Orthotopicglioblastomamousemodel[5]Dosage:80mg/kgAdministration:Oralgavage,for3days.Result:Reducestumorsize(MRimaging)andimprovesinoverallsurvival.REFERENCES[1].E.MarcJolicoeur,etal.27-RefractoryAngina.ChronicCoronaryArteryDisease,2018,412-431.[2].ZhenRen,etal.Mitochondrialdysfunctionandapoptosisunderliethehepatotoxicityofperhexiline.ToxicolInVitro.2020Dec;69:104987.[3].P-PLiu,etal.EliminationofchroniclymphocyticleukemiacellsinstromalmicroenvironmentbytargetingCPTwithanantianginadrugperhexiline.Oncogene.2016Oct27;35(43):5663-5673.[4].GiovanniLicari,etal.Enantioselectivityinthetissuedistributionofperhexilinecontributestodifferenteffectsonhepatichistologyandperipheralneuralfunctioninrats.PharmacolResPerspect.2018Jun;6(3):e00406.[5].ShivaKant,etal.PerhexilineDemonstratesFYN-mediatedAntitumorActivityinGlioblastoma.MolCancerTher.2020Jul;19(7):1415-1422.McePdfHeightCauti