Nevanimibe-hydrochloride-PD-132301-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENevanimibehydrochlorideCat.No.:HY-100399ACASNo.:133825-81-7Synonyms:PD-132301hydrochloride;ATR101hydrochloride分?式:C??H??ClN?O分?量:458.08作?靶點(diǎn):Acyltransferase;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(shí)驗(yàn)DMSO:41.67mg/mL(90.97mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1830mL10.9151mL21.8302mL5mM0.4366mL2.1830mL4.3660mL10mM0.2183mL1.0915mL2.1830mL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?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)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(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%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.54mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.54mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.54mM);ClearsolutionBIOLOGICALACTIVITY?物活性Nevanimibehydrochloride(PD-132301hydrochloride)?種?服有效的，選擇性酰輔酶A：膽醇O-酰1(ACAT1)抑制劑，EC50為9nM。Nevanimibehydrochloride抑制ACAT2，EC50為368nM[1]。Nevanimibehydrochloride誘導(dǎo)細(xì)胞凋亡(apoptosis)，并具有抗腎上腺?質(zhì)癌的潛?。IC50&TargetACAT1ACAT29nM(EC50)368nM(EC50)體外研究CoincubationofNevanimibehydrochloride(PD-132301hydrochloride;ATR101hydrochloride;3nM-30μM)andCholesterolmarkedlyincreasestoxicityinadose-dependentmanner,where3nMNevanimibeinthepresenceof60μg/mLCholesterolreducessurvivalby60%after24hours.AlldosesofNevanimibe(3nM-30μM)inducescytoxicityinthepresenceofCholesterol,whereastreatmentwithCholesterolintheabsenceofNevanimibehasnoeffectoncellviability[1].CellCytotoxicityAssay[1]CellLine:TheH295RandHACclone15(HAC15)humanACCcelllinesConcentration:3nM-30μMIncubationTime:24hoursResult:3nM-3μMexhibitednotoxicity,whereas30μMtreatmentreducedsurvivalbyapproximately40%within24hours.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Structure.2021Sep11;S0969-2126(21)00259-8.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LaPenseeCR,etal.ATR-101,aSelectiveandPotentInhibitorofAcyl-CoAAcyltransferase1,InducesApoptosisinH295RAdrenocorticalCellsandintheAdrenalCortexofDogs.Endocrinology.2016May;157(5):1775-88.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedical