Statil-Ponalrestat-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEStatilCat.No.:HY-106697CASNo.:72702-95-5Synonyms:Ponalrestat分⼦式:C₁₇H₁₂BrFN₂O₃分⼦量:391.19作⽤靶点:AldoseReductase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:62.5mg/mL(159.77mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5563mL12.7815mL25.5630mL5mM0.5113mL2.5563mL5.1126mL10mM0.2556mL1.2782mL2.5563mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.32mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性Statil(Ponalrestat)⼀种具有⼝服活性，选择性和⾮竞争性的醛糖还原酶(aldosereductase；AKR1B1；ALR)抑制剂。Statil可以选择性抑制ALR2，Ki为7.7nM，对ALR1的Ki值为60μM。Statil抑制葡萄糖向⼭梨糖醇的转化。IC50&TargetKi:7.7nM(ALR2)and60μM(ALR1)[1]体外研究Statil(Ponalrestat;1,10,100μM;6hours)reducesPGF2αproductioninresponsetoIL-1inbothculturedendometrialcellsandendometrialexplants[2].体内研究Statil(Ponalrestat;10,50mg/kg;orally;daily;8weeks)reducessorbitolaccumulationindicatingefficacyofaldosereductaseinhibition[3].AnimalModel:AdultfemaleSprague-Dawleyrats[3]Dosage:10,50mg/kgAdministration:Orally;daily;8weeksResult:Reducedsorbitolaccumulation.REFERENCES[1].WardWH,etal.Ponalrestat:apotentandspecificinhibitorofaldosereductase.BiochemPharmacol.1990Jan15;39(2):337-46.[2].BressonE,etal.ThehumanaldosereductaseAKR1B1qualifiesastheprimaryprostaglandinFsynthaseintheendometrium.JClinEndocrinolMetab.2011Jan;96(1):210-9.[3].CalcuttNA,etal.PreventionofsensorydisordersindiabeticSprague-Dawleyratsbyaldosereductaseinhibitionortreatmentwithciliaryneurotrophicfactor.Diabetologia.2004Apr;47(4):718-24.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T