Fezagepras-sodium-Setogepram-sodium-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFezageprassodiumCat.No.:HY-100775CASNo.:1254472-97-3Synonyms:Setogepramsodium;PBI-4050sodium分⼦式:C₁₃H₁₇NaO₂分⼦量:228.26作⽤靶点:FreeFattyAcidReceptor;GPR84作⽤通路:GPCR/GProtein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H2O:≥100mg/mL(438.10mM)DMSO:≥64mg/mL(280.38mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM4.3810mL21.9048mL43.8097mL5mM0.8762mL4.3810mL8.7619mL10mM0.4381mL2.1905mL4.3810mL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)1/3MasterofBioactiveMolecules—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(9.11mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(9.11mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(9.11mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:120mg/mL(525.72mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Fezagepras(Setogepram)sodium⼀种具有⼝服活性的GPR40激动剂和GPR84拮抗剂或反向激动剂[1]。Fezageprassodium减轻肾，肝和胰腺纤维化[1][2]。Fezageprassodium具有抗纤维化，抗炎和抗增殖作⽤[2]。IC50&TargetGPR40,GPR84[1]体外研究Fezageprassodium(500µM;24hours)inhibitsTGF-β(10ng/mL)-activatedhumanhepaticstellatecells(HSCs)proliferation[2].Fezageprassodium(250or500µM;24hours)dose-dependentlyarrestsHSCsattheG0/G1phasewithoutinducingapoptosis[2].CellProliferationAssay[2]CellLine:HSCsConcentration:250or500µMIncubationTime:24hoursResult:InhibitedTGF-β-activatedHSCproliferation.TGF-β(10ng/mL)increasedHSCproliferationby10%.CellCycleAnalysis[2]CellLine:HSCsConcentration:250µM,500µMIncubationTime:24hoursResult:Inhibitedcellcycleprogression.体内研究Fezageprassodium(100mg/kg/day;gavagefrom8-20weeksofage)markedlydecreaseshyperglycemiaandmarkedlyimproveaglucosetoleranceintype2diabeteseNOS-/-db/dbmice[1].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Type2diabeteseNOS-/-db/dbmice[1]Dosage:100mg/kg/dayAdministration:Givenviadailygavagefrom8-20weeksResult:Comparedwithvehicle-treatedmice,hyperglycemiawasmarkedlydecreased,andglucosetolerancewasmarkedlyimproved.REFERENCES[1].LiY,etal.FattyacidreceptormodulatorPBI-4050inhibitskidneyfibrosisandimprovesglycemiccontrol.JCIInsight.2018May17;3(10).pii:120365.[2].GrouixB,etal.PBI-4050ReducesStellateCellActivationandLiverFibrosisthroughModulationofIntracellularATPLevelsandtheLiverKinaseB1/AMP-ActivatedProteinKinase/MammalianTargetofRapamycinPathway.JPharmacolExpTher.2018Oct;367(1):McePdfHeightCaution:Producthasnotbeenfullyvali