Tolmetin-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemETolmetinCat.No.:HY-B1799CASNo.:26171-23-3分⼦式:C₁₅H₁₅NO₃分⼦量:257.28作⽤靶点:COX作⽤通路:Immunology/Inflammation储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:100mg/mL(388.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.8868mL19.4341mL38.8682mL5mM0.7774mL3.8868mL7.7736mL10mM0.3887mL1.9434mL3.8868mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(9.72mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(9.72mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(9.72mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Tolmetin⼀种具有⼝服活性的，有效的COX抑制剂，对⼈COX-1和COX-2的IC50值分别为0.35µM和0.82µM。Tolmetin属于⾮甾体类物质，具有强效的抗炎活性。IC50&TargetHumanCOX-1HumanCOX-20.35μM(IC50)0.82μM(IC50)体外研究Tolmetin(0.25mM)doesnotattenuatelipidperoxidationinratbrainhomogenate.Tolmetin(0.25,0.5,0.75,1mM)showsradicalscavengingpropertiesbutwithoutsuperoxideaniongenerationinratbrainhomogenat[3].Tolmetin(0.001-100μM)showsanticanceractivityagaintsHT-29coloncancercelllineinadose-dependentmanner[4].Tolmetin(0-100μM)showsnoeffectonosteoblastgrowth[5].体内研究Tolmetin(30,100mg/kg;gavage;singledoseortwicedailyfor3and14days)showsmaximalulcerogeniceffect4hafterthesingledose,whilepotentlydecreasesafter3and14daysofrepeatedadministrationinmaleWistarratsweighing180-200g.Tolmetincausesgastriclesionsin100mg/kg[2].Tolmetin(5mg/kgtwiceadayfor5days)pre-treatmentconsiderablyattenuatesquinolinicacid(QA)-inducedneurotoxicity[3].REFERENCES[1].TDWarner,etal.Nonsteroiddrugselectivitiesforcyclo-oxygenase-1ratherthancyclo-oxygenase-2areassociatedwithhumangastrointestinaltoxicity:afullinvitroanalysis.ProcNatlAcadSciUSA.1999Jun22;96(13):7563-8.[2].DADAŞ,Yakup,etal.Synthesisandanticanceractivityofsomenoveltolmetinthiosemicarbazides.MarmaraPharmaceuticalJournal19(3)•April2015[3].EtcheverrySB,etal.Threenewvanadyl(IV)complexeswithnon-steroidalanti-inflammatorydrugs(Ibuprofen,NaproxenandTolmetin).Bioactivityonosteoblast-likecellsinculture.JInorgBiochem.2002Jan1;88(1):94-100.[4].EtcheverrySB,etal.Threenewvanadyl(IV)complexeswithnon-steroidalanti-inflammatorydrugs(Ibuprofen,NaproxenandTolmetin).Bioactivityonosteoblast-likecellsinculture.JInorgBiochem.2002Jan1;88(1):94-100.[5].EtcheverrySB,etal.Threenewvanadyl(IV)complexeswithnon-steroidalanti-inflammatorydrugs(Ibuprofen,NaproxenandTolmetin).Bioactivityonosteoblast-likecellsinculture.JInorgBiochem.2002Jan1;88(1):94-100.McePdfHeightCaution:Producthasnotbeenfullyv