APX-115-Ewha-18278-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAPX-115Cat.No.:HY-120801CASNo.:1395946-75-4Synonyms:Ewha-18278分?式:C??H??ClN?O分?量:315.8作?靶點:NADPHOxidase作?通路:MetabolicEnzyme/Protease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DMSO:100mg/mL(316.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1666mL15.8328mL31.6656mL5mM0.6333mL3.1666mL6.3331mL10mM0.3167mL1.5833mL3.1666mL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?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%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.59mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.59mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.59mM);ClearsolutionBIOLOGICALACTIVITY?物活性APX-115(Ewha-18278)?種有效的，?服活性的，?選擇性Nox抑制劑，對Nox1，Nox2和Nox4的Ki值分別為1.08μM，0.57μM和0.63μM。APX-115可有效預防糖尿病??的腎損傷。IC50&TargetKi:1.08μM(Nox1),0.57μM(Nox2)and0.63μM(Nox4)[1]體外研究APX-115(5?μM;60?min)almostcompletelysuppresseshighglucose-inducedproinflammatoryandprofibroticmoleculeexpressioninthemousepodocytecellline[2].Inthekidney,APX-115attenuatesNoxgeneupregulationandproteinexpressionwhileimprovinginflammatoryandfibroticprocesses[2].體內(nèi)研究APX-115(oralgavage;60?mg/kg/day;for12weeks)significantlyimprovesinsulinresistanceindiabeticmice[2].APX-115treatmentdecreasestheurinaryexcretionofalbuminandplasmacreatininelevels[2].AnimalModel:Six-week-oldmalediabeticdb/dbmice(C57BLKS/J-leprdb/leprdb)[2]Dosage:60?mg/kgAdministration:Oralgavage;perday;for12weeksResult:Significantlyimprovedinsulinresistanceindiabeticmice.戶使?本產(chǎn)品發(fā)表的科研?獻?NatImmunol.2021Sep;22(9):1107-1117.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KwonG,etal.Anovelpan-Noxinhibitor,APX-115,protectskidneyinjuryinstreptozotocin-induceddiabeticmice:possibleroleofperoxisomalandmitochondrialbiogenesis.Oncotarget.2017Jun16;8(43):74217-74232.[2].ChaJJ,etal.APX-115,afirst-in-classpan-NADPHoxidase(Nox)inhibitor,protectsdb/dbmicefromrenalinjury.LabInvest.2017Apr;97(4):419-431.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalap