FPTQ-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFPTQCat.No.:HY-100382CASNo.:864863-72-9分⼦式:C₁₇H₁₂FN₅分⼦量:305.31作⽤靶点:mGluR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:33.33mg/mL(109.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2754mL16.3768mL32.7536mL5mM0.6551mL3.2754mL6.5507mL10mM0.3275mL1.6377mL3.2754mL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(8.19mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性FPTQ⼀种有效的mGluR1拮抗剂，抑制⼈和⿏的IC50值分别为6nM和1.4nM。FPTQ具有抗氧化、抗炎作⽤。IC50&TargetHumanmGluR1MousemGluR16nM(IC50)1.4nM(IC50)体外研究FPTQ(0.5-10μM)doesnotshowsanycytotoxicitywasnotobservedat0.5,1,5,and10μMinRAW264.7macrophagecells[2].FPTQ(1-20μM;24hours)reducesLPS-inducedNOproductionat>1μMFPTQ,andat10μM,FPTQtreatmentcausesa31%anti-oxidanteffectinRAW264.7macrophagecells[2].FPTQ(1-20μM;24hours)dramaticlydecreasesLPS-inducedexpressionlevelsofIL-1βandIl-6.Ataconcentrationof10μM,FPTQcausesa27%and44%reductioninthemRNAexpressionofIL-1βandIl-6,respectivelyinRAW264.7macrophagecells[2].RT-PCR[1]CellLine:RAW264.7macrophagecellsConcentration:1,10,or20μMIncubationTime:24hoursResult:DecreasedIL-1βandIL-6mRNAexpression体内研究FPTQ(5-20μM)decreasesthenumberofneutrophilsmigratingtotheamputationsiteinzebrafishlarvaebytailamputation.Inthetailfinwoundmethod,thenumberofneutrophilscollectingatthewoundsitealsodecreasesinadose-dependentmannerinzebrafish[2].InaLPS-inducedinflammationzebrafishmodel,LPSsolutionisinjectedintotheyolksofTg(mpx:EGFP)i114zebrafishlarvaeandexposedthezebrafishlarvaeimmediatelytoFPTQtreatment.FPTQ(20μM;4hours)significantlydecreasesthefluorescentneutrophilsafteryolkinjectionandhasananti-inflammatoryeffectduringtheearlyphaseofinflammation[2].REFERENCES[1].FujinagaMetal.Synthesisandevaluationof6-[1-(2-[(18)F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinolineforpositronemissiontomographyimagingofthemetabotropicglutamatereceptortype1inbrain.BioorgMedChem,2011Jan1,19(1):102[2].GeumRanKim,etal.Anti-inflammatoryeffectofanovelsyntheticcompound1-((4-fluorophenyl)thio)isoquinolineinRAW264.7macrophagesandazebrafishmodel.FishShellfishImmunol.2019Apr;87:395-400.McePdfHeightCaution:Producthasnotbeenfullyvalidatedforme