Perhexiline-maleate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPerhexilinemaleateCat.No.:HY-B1334ACASNo.:6724-53-4分?式:C??H??NO?分?量:393.56作?靶點(diǎn):MitochondrialMetabolism;Apoptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗Ethanol:20mg/mL(50.82mM;Needultrasonic)DMSO:3.57mg/mL(9.07mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5409mL12.7045mL25.4091mL5mM0.5082mL2.5409mL5.0818mL10mM0.2541mL1.2705mL2.5409mL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；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?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：(為保證實驗結(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)實驗的?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%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥0.5mg/mL(1.27mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥0.5mg/mL(1.27mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥0.5mg/mL(1.27mM);Clearsolution4.請依序添加每種溶劑：10%EtOH>>90%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(5.08mM);ClearsolutionBIOLOGICALACTIVITY?物活性Perhexilinemaleate?種具有?服活性的CPT1和CPT2抑制劑，可減少脂酸代謝。Perhexilinemaleate在肝細(xì)胞中誘導(dǎo)線粒體功能障礙和細(xì)胞凋亡(apoptosis)。Perhexilinemaleate可穿過?腦屏障(BBB)，并顯?出抗腫瘤活性。Perhexilinemaleate可?于癌癥和?絞痛等??管疾病的研究。IC50&TargetIC50:77μM(RatheartCPT1),148μM(RatliverCPT1)[1]體外研究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.體內(nèi)研究Perhexiline(200mg/kg,p.o.,dailyfor8weeks)maleatereducesperipheralneuralfunctioninfemaleDArats[4].Perhexiline(80mg/kg,oralgavage,for3days)maleatedemonstratesanti-tumoractivityinglioblastomamousemodel[5].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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