Indomethacin-sodium-hydrate-Indometacin-sodium-hydrate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEIndomethacinsodiumhydrateCat.No.:HY-14397ACASNo.:74252-25-8Synonyms:Indometacinsodiumhydrate分?式:C??H??ClNNaO?分?量:433.82作?靶點(diǎn):COX;Autophagy作?通路:Immunology/Inflammation;Autophagy儲(chǔ)存?式:4°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:33.33mg/mL(76.83mM;Needultrasonic)DMSO:5mg/mL(11.53mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3051mL11.5255mL23.0510mL5mM0.4610mL2.3051mL4.6102mL10mM0.2305mL1.1526mL2.3051mL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，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。BIOLOGICALACTIVITY?物活性Indomethacinsodiumhydrate(Indometacinsodiumhydrate)?種有效的，可透過(guò)?腦屏障的，?選擇性的COX1和COX2抑制劑，在CHO細(xì)胞中，對(duì)?COX-1和COX-2的IC50值分別為18nM和26nM[1]。Indomethacinsodiumhydrate通過(guò)?擾溶酶體的正常功能來(lái)破壞?噬流(autophagicflux)[1]。體外研究IndomethacinisapotentandnonselectiveinhibitorofCOX1andCOX2,withIC50sof18nMand26nMforhumanCOX-1andCOX-2,respectively,inCHOcells.Indomethacininhibitslipopolysaccharide(LPS)-1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEinducedPGE2production(COX-2)inahumanwholebloodassaywithapotency(IC50=0.68±0.17?μM),andsuppressescoagulation-inducedTXB2production(COX-1)(IC50=0.19±0.02?μM).IndomethacinblocksCOX-1withanIC50of20±1?nMinU937cellmicrosomesatalowarachidonicacidconcentration(0.1?μM)[1].體內(nèi)研究Indomethacindose-dependentlyinhibitsboththecarrageenan-inducedratpawoedema(ED50,2.0?mg/kg),hyperalgesia(ED50,1.5?mg/kg),andisalsoeffectiveatreversingLPS-inducedpyrexiainrats(ED50,1.1?mg/kg)[1].Indomethacin(2.5mg/kg,i.p)decreasesthenumberofNeuN+cellsintheanimalsat8daysafterET-1injection.Indomethacinalsoreducesmicroglia/macrophageactivationat14days.IndomethacinsignificantlyincreasesthenumberofSVZDCX+cells/fieldat14dayspoststroke[3].Indomethacin(22.9mg/kg,p.o.)produces8to10linearmucosallesionsextendedfromthefundictopyloricareaofstomachwall[4].?ChemMater.2017,29(19):8221-8238.?IntJNanomedicine.2020May1;15:3087-3098.?IntJPharm.2017Jan30;517(1-2):19-24.?Langmuir.2020Sep9.?ToxicolApplPharmacol.2017Mar22;323:44-52.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RiendeauD,etal.BiochemicalandpharmacologicalprofileofatetrasubstitutedfuranoneasahighlyselectiveCOX-2inhibitor.BrJPharmacol.1997May;121(1):105-17.[2].JorgeVallecillo-Hernández,etal.IndomethacinDisruptsAutophagicFluxbyInducingLysosomalDysfunctioninGastricCancerCellsandIncreasesTheirSensitivitytoCytotoxicDrugs.SciRep.2018Feb26;8(1):3593.[3].LopesRS,etal.Indomethacintreatmentreducesmicrogliaactivationandincreasesnumbersofneuroblastsinthesubventricularzoneandischaemicstriatumafterfocalischaemia.JBiosci.2016Sep;41(3):381-94.[4].AfrozS,etal.Concentratedphosphatidicacidincerealbransaspotentialprotectiveagentsagainstindomethacin-inducedstomachulcer.JAgricFoodChem.2016Aug26.McePdfHeightCaution:Producthasnotbeenfully