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

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAPX-115freebaseCat.No.:HY-120801ACASNo.:1270084-92-8Synonyms:Ewha-18278freebase分⼦式:C₁₇H₁₇N₃O分⼦量:279.34作⽤靶点:NADPHOxidase作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(894.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5799mL17.8993mL35.7987mL5mM0.7160mL3.5799mL7.1597mL10mM0.3580mL1.7899mL3.5799mL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。-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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(7.45mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.45mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.45mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性APX-115freebase(Ewha-18278freebase)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-115freebase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-115freebase(5ꢀμM;60ꢀmin)almostcompletelysuppresseshighglucose-inducedproinflammatoryandprofibroticmoleculeexpressioninthemousepodocytecellline[2].Inthekidney,APX-115freebaseattenuatesNoxgeneupregulationandproteinexpressionwhileimprovinginflammatoryandfibroticprocesses[2].体内研究APX-115freebase(oralgavage;60ꢀmg/kg/day;for12weeks)significantlyimprovesinsulinresistanceindiabeticmice[2].APX-115freebasetreatmentdecreasestheurinaryexcretionofalbuminandplasmacreatininelevels[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):419-431.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap