Firuglipel-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFiruglipelCat.No.:HY-109032CASNo.:1371591-51-3分?式:C??H??FN?O?分?量:467.49作?靶點(diǎn):GPR119作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(213.91mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1391mL10.6954mL21.3908mL5mM0.4278mL2.1391mL4.2782mL10mM0.2139mL1.0695mL2.1391mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.35mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.35mM);ClearsolutionBIOLOGICALACTIVITY?物活性Firuglipel(DS-8500a)?效，選擇性，有?服活性的GPR119激動(dòng)劑。IC50&TargetGPR119[1]體外研究Firuglipel(DS-8500a)increasesintracellularcAMPinaconcentration-dependentmannerinhuman,rat,andmouseGPR119-expressingChinesehamsterovary(CHO)-K1cells,withEC50valuesof51.5,98.4,and108.1nM,respectively.DS-8500ahasnoeffectonintracellularcAMPinpcDNA3.1/CHO-K1cells[1].體內(nèi)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