Auranofin-SKF-39162-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAuranofinCat.No.:HY-B1123CASNo.:34031-32-8Synonyms:SKF-39162分?式:C??H??AuO?PS分?量:680.5作?靶點(diǎn):Bacterial;SARS-CoV作?通路:Anti-infection儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(73.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.4695mL7.3475mL14.6951mL5mM0.2939mL1.4695mL2.9390mL10mM0.1470mL0.7348mL1.4695mL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(sealedstorage,awayfrommoisture)。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.67mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(3.06mM);Suspendedsolution;Needultrasonicandwarming3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.06mM);ClearsolutionBIOLOGICALACTIVITY?物活性Auranofin(SKF-39162)硫氧還蛋?還原酶(TrxR)的抑制劑，IC50為0.2μM。Auranofin表現(xiàn)出抗SARS-CoV21的抗病毒活性，對猴腎VeroE6細(xì)胞的CC50為4.2μM。IC50&TargetIC50:0.2μM(TrxR)[1]體外研究Auranofinisadrugthatisapprovedforthetreatmentofrheumatoidarthritisbutisbeinginvestigatedforpotentialtherapeuticapplicationinanumberofotherdiseasesincludingcancer,neurodegenerativedisorders.AuranofininducesapoptosisincellsthroughaBax/Bak-dependentmechanismassociatedwithselectivedisruptionofmitochondrialredoxhomeostasisinconjunctionwithoxidationofPrx3[1].AuranofininhibitsproliferationandsurvivalofSKOV3cellsinadose-andtime-dependentmanner.Auranofintreatmentactivatesthepro-apoptoticcaspase-3,increasesproteinlevelsofapoptosis-inducingproteinsBaxandBimandreducestheexpressionoftheanti-apoptoticmediatorBcl-2inSKOV3cells[2].Auranofinisalipophilicgoldcompoundwithanti-inflammatoryandimmunosuppressiveproperties.AuranofininhibitsthecellgrowthandinductionofmitochondrialapoptosisinPC3humanprostatecancercells.TreatmentwithauranofinsignificantlyinhibitscellviabilitywithanIC50valueof2.5μMafter24h[3].體內(nèi)研究Prophylactictreatmentofadjuvant-inducedarthritisratswithauranofinresultsinaslightreductioninpawedema,acompletenormalizationofthedepressedIL-2production,andareductionoftheelevatedIL-1production,buthasnoeffectonthedepressedIL-3production[4].PROTOCOLCellAssay[2]AuranofinisdissolvedinDMSO.Cellsaretreatedwithauranofin(0,50,100,200and400nM)for72hforthedose-dependentresponseassayand100nMofauranofinisaddedintothewellsfor0,24,72and120hforthetime-dependentresponseassay.ControlculturesaretreatedwithDMSO.CellviabilityismeasuredbytheMTTassay[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRats:Prophylactically,auranofin(6.7to15mgofgold/kg),indomethacin(2mg/kg)ortragacanthvehicleAdministration[4]controlwereadministeredorallyatdailyintervalsbeginningonthedayofadjuvantinjection.Ondays16to17peritonealexudatecellsorspleencellsfromnormaloradjuvant-injectedratswereisolatedandtested[4].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?NatMicrobiol.2020Nov;5(11):1439-1448.?NucleicAcidsRes.2021Jan8;49(D1):D1113-D1121.?NatCommun.2020Oct16;11(1):5263.?CellDeathDiffer.2020Mar;27(3):1086-1104.?RedoxBiol.2020Sep;36:101652.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CoxAG,etal.ThethioredoxinreductaseinhibitorauranofintriggersapoptosisthroughaBax/Bak-dependentprocessthatinvolvesperoxiredoxin3oxidation.BiochemPharmacol.2008Oct30;76(9):1097-109.[2].ParkSH,etal.AuranofindisplaysanticanceractivityagainstovariancancercellsthroughFOXO3activationindependentofp53.IntJOncol.2014Oct;45(4):1691-8.[3].ParkN,etal.AuranofinpromotesmitochondrialapoptosisbyinducingannexinA5expressionandtranslocationinhumanprostatecancercells.JToxicolEnvironHealthA.2014;77(22-24):1467-76.[4].LeeJC,etal.Effectofauranofintreatmentonaberrantsplenicinterleukinproductioninadjuvantarthriticrats.JImmunol.1987Nov15;139(10):3268-74.[5].ShuofengYuan,etal.MetallodrugranitidinebismuthcitratesuppressesSARS-CoV-2replicationandrelievesvirus-associatedpneumoniainSyria