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

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMofezolacCat.No.:HY-120824CASNo.:78967-07-4分?式:C??H??NO?分?量:339.34作?靶點:COX作?通路:Immunology/Inflammation儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(294.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9469mL14.7345mL29.4690mL5mM0.5894mL2.9469mL5.8938mL10mM0.2947mL1.4734mL2.9469mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.37mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.37mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.37mM);ClearsolutionBIOLOGICALACTIVITY?物活性Mofezolac，?種?甾體類抗炎藥(NSAID)，?種選擇性，可逆和具有?服活性的COX-1抑制劑，IC50為1.44nM。Mofezolac對COX-2的抑制活性較弱(IC50為447nM)。Mofezolac可緩解疼痛并具有抗炎活性。IC50&TargetCOX-1COX-21.44nM(IC50)447nM(IC50)體外研究MofezolacinhibitsplateletaggregationwithanIC50of0.45μMinhumanplateletrichplasma(hPRP)assay[2].MofezolacslightlyincreaseBortezomibcytotoxiceffectonmultiplemyeloma(MM)celllines(NCI-H929andRPMI-8226)andaffectsMMcellcycleandapoptosiswhenco-administeredwiththeproteasomeinhibitorBortezomib[2].體內(nèi)研究Mofezolac(1-30mg/kg;oraladministration;once)treatmentresultsinthesuppressionofwrithinginducedbytheintraperitonealinjectionofphenyl-p-benzoquinoneinmice[1].AnimalModel:FemaleddYmice(4weekold,18-27g)injectedwithphenyl-p-benzoquinone(PQ)[1]Dosage:1mg/kg,3mg/kg,10mg/kg,30mg/kgAdministration:Oraladministration;onceResult:Dose-dependentlysuppressedthewrithinginducedbyPQinjectioninmice.REFERENCES[1].KGoto,etal.Analgesiceffectofmofezolac,anon-steroidalanti-inflammatorydrug,againstphenylquinone-inducedacutepaininmice.ProstaglandinsOtherLipidMediat.1998Jul;56(4):245-54.[2].MariaLauraPati,etal.Translationalimpactofnovelwidelypharmacologicalcharacterizedmofezolac-derivedCOX-1inhibitorscombinedwithbortezomibonhumanmultiplemyelomacelllinesviability.EurJMedChem.2019Feb15;164:59-76.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplication