GSK2256294A-GSK-2256294-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK2256294ACat.No.:HY-19644CASNo.:1142090-23-0Synonyms:GSK2256294分⼦式:C₂₁H₂₄F₃N₇O分⼦量:447.46作⽤靶点:EpoxideHydrolase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:≥47mg/mL(105.04mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2348mL11.1742mL22.3484mL5mM0.4470mL2.2348mL4.4697mL10mM0.2235mL1.1174mL2.2348mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.65mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.65mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.65mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GSK2256294A(GSK2256294)⼀种选择性的，以及⼝服活性的solubleepoxidehydrolase(sEH)抑制剂。GSK2256294A对⼈的重组sEH、⼤⿏同sEH和⼩⿏同sEH具有抑制作⽤，其IC50值分别为27、61和189pM。GSK2256294A可⽤于慢性阻塞性肺疾病(COPD)和⼼⾎管疾病的研究。IC50&TargetIC50:27pM(recombinanthumansEH),61pM(ratsEHorthologs),189pM(murinesEHorthologs)[1]体外研究GSK2256294A(300pM-10μM;2h)inhibitstheconversionof14,15-EET-d11to14,15-DHET-d11inhuman,ratandmousewholeblood[1].体内研究GSK2256294A(5-30mg/kg;p.o.twicedaily5days/weekfortwoweeks)inhibitsthegenerationandmaintenanceofpulmonaryinflammationincigarettesmoke-exposedmice[1].GSK2256294A(30mg/kg;p.o.twicedailyfor8days)decreasespulmonaryinflammationincigarettesmoke-exposedmice[1].AnimalModel:Miceexposedtocigarettesmoke5days/weekfor2weeks[1]Dosage:5and30mg/kgAdministration:Oralgavage;5and30mg/kgtwicedaily5days/week;for2weeksResult:Dose-dependentlyinhibitednumbersofBALfluidtotalcells,neutrophils,macrophagesandthekeratinocytechemoattractant(KC)levelsinlungtissue.AnimalModel:Miceexposedtocigarettesmoke5days/weekfor2weeks[1]Dosage:30mg/kgAdministration:Oralgavage;30mg/kgtwicedaily;for8daysResult:Significantlyreducedneutrophils,macrophagesandpulmonaryinflammationincigarettesmoke-exposedmice.户使⽤本产品发表的科研⽂献•Diabetes.2018Jun;67(6):1162-1172.•UniversidadElBosque.MariaFernandaSalazarRomero.2022May.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].PodolinPL,etal.Invitroandinvivocharacterizationofanovelsolubleepoxidehydrolaseinhibitor.ProstaglandinsOtherLipidMediat.2013Jul-Aug;104-105:25-31.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor