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

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFPTQCat.No.:HY-100382CASNo.:864863-72-9分?式:C??H??FN?分?量:305.31作?靶點(diǎn):mGluR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:33.33mg/mL(109.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.2754mL16.3768mL32.7536mL5mM0.6551mL3.2754mL6.5507mL10mM0.3275mL1.6377mL3.2754mL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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/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(8.19mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性FPTQ?種有效的mGluR1拮抗劑，抑制?和?的IC50值分別為6nM和1.4nM。FPTQ具有抗氧化、抗炎作?。IC50&TargetHumanmGluR1MousemGluR16nM(IC50)1.4nM(IC50)體外研究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體內(nèi)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