Firuglipel-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFiruglipelCat.No.:HY-109032CASNo.:1371591-51-3分⼦式:C₂₅H₂₆FN₃O₅分⼦量:467.49作⽤靶点:GPR119作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(213.91mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1391mL10.6954mL21.3908mL5mM0.4278mL2.1391mL4.2782mL10mM0.2139mL1.0695mL2.1391mL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%salineSolubility:≥2.5mg/mL(5.35mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.35mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Firuglipel(DS-8500a)⾼效，选择性，有⼝服活性的GPR119激动剂。IC50&TargetGPR119[1]体外研究Firuglipel(DS-8500a)increasesintracellularcAMPinaconcentration-dependentmannerinhuman,rat,andmouseGPR119-expressingChinesehamsterovary(CHO)-K1cells,withEC50valuesof51.5,98.4,and108.1nM,respectively.DS-8500ahasnoeffectonintracellularcAMPinpcDNA3.1/CHO-K1cells[1].体内研究Firuglipel(DS-8500a)(1-30mg/kg)upregulatesglucagon-likepeptide-1andenhancesglucose-dependentinsulinsecretionandimprovesglucosehomeostasisintype2diabeticrats[1].PROTOCOLAnimalRats[1]Administration[1]MaleSDrats(8weeks)arefastedovernightandorallygivenvehicle(0.5%MC),DS-8500a(0.1,1,3and10mg/kg),orglimepiride(10mg/kg).Thirtyminuteslater,allanimalsreceiveda50%glucosesolutionintravenously(glucoseload:0.5g/kg).Bloodcollectionisperformedfromthetailvein35minutesbefore,5minutesbefore,and5minutesaftertheglucoseload.TheplasmainsulinconcentrationismeasuredusingELISAkits.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].MatsumotoK,etal.DS-8500a,anOrallyAvailableGProtein-CoupledReceptor119Agonist,UpregulatesGlucagon-LikePeptide-1andEnhancesGlucose-DependentInsulinSecretionandImprovesGlucoseHomeostasisinType2DiabeticRats.JPharmacolExpTher.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo