Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFezageprassodiumCat.No.:HY-100775CASNo.:1254472-97-3Synonyms:Setogepramsodium;PBI-4050sodium分?式:C??H??NaO?分?量:228.26作?靶點:FreeFattyAcidReceptor;GPR84作?通路:GPCR/GProtein儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數據體外實驗H2O:≥100mg/mL(438.10mM)DMSO:≥64mg/mL(280.38mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.3810mL21.9048mL43.8097mL5mM0.8762mL4.3810mL8.7619mL10mM0.4381mL2.1905mL4.3810mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(9.11mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(9.11mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(9.11mM);Clearsolution4.請依序添加每種溶劑：PBSSolubility:120mg/mL(525.72mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Fezagepras(Setogepram)sodium?種具有?服活性的GPR40激動劑和GPR84拮抗劑或反向激動劑[1]。Fezageprassodium減輕腎，肝和胰腺纖維化[1][2]。Fezageprassodium具有抗纖維化，抗炎和抗增殖作?[2]。IC50&TargetGPR40,GPR84[1]體外研究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.體內研究Fezageprassodium(100mg/kg/day;gavagefrom8-20weeksofage)markedlydecreaseshyperglycemiaandmarkedlyimproveaglucosetoleranceintype2diabeteseNOS-/-db/dbmice[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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