APX-115-Ewha-18278-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAPX-115Cat.No.:HY-120801CASNo.:1395946-75-4Synonyms:Ewha-18278分⼦式:C₁₇H₁₈ClN₃O分⼦量:315.8作⽤靶点:NADPHOxidase作⽤通路:MetabolicEnzyme/Protease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DMSO:100mg/mL(316.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1666mL15.8328mL31.6656mL5mM0.6333mL3.1666mL6.3331mL10mM0.3167mL1.5833mL3.1666mL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:≥2.08mg/mL(6.59mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.59mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.59mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性APX-115(Ewha-18278)⼀种有效的，⼝服活性的，⾮选择性Nox抑制剂，对Nox1，Nox2和Nox4的Ki值分别为1.08μM，0.57μM和0.63μM。APX-115可有效预防糖尿病⼩⿏的肾损伤。IC50&TargetKi:1.08μM(Nox1),0.57μM(Nox2)and0.63μM(Nox4)[1]体外研究APX-115(5ꢀμM;60ꢀmin)almostcompletelysuppresseshighglucose-inducedproinflammatoryandprofibroticmoleculeexpressioninthemousepodocytecellline[2].Inthekidney,APX-115attenuatesNoxgeneupregulationandproteinexpressionwhileimprovinginflammatoryandfibroticprocesses[2].体内研究APX-115(oralgavage;60ꢀmg/kg/day;for12weeks)significantlyimprovesinsulinresistanceindiabeticmice[2].APX-115treatmentdecreasestheurinaryexcretionofalbuminandplasmacreatininelevels[2].AnimalModel:Six-week-oldmalediabeticdb/dbmice(C57BLKS/J-leprdb/leprdb)[2]Dosage:60ꢀmg/kgAdministration:Oralgavage;perday;for12weeksResult:Significantlyimprovedinsulinresistanceindiabeticmice.户使⽤本产品发表的科研⽂献•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—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalap