Chloroquine-phosphate-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEChloroquinephosphateCat.No.:HY-17589CASNo.:50-63-5分?式:C??H??ClN?O?P?分?量:515.86作?靶點:Parasite;Autophagy;SARS-CoV;Toll-likeReceptor(TLR);HIV;Antibiotic作?通路:Anti-infection;Autophagy;Immunology/Inflammation儲存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實驗H2O:≥33mg/mL(63.97mM)DMSO:<1mg/mL(ultrasonic)(insolubleorslightlysoluble)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9385mL9.6926mL19.3851mL5mM0.3877mL1.9385mL3.8770mL10mM0.1939mL0.9693mL1.9385mL請根據(jù)產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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：PBS1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:100mg/mL(193.85mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY?物活性Chloroquinephosphate?種?泛?于瘧疾和類風濕性關節(jié)炎的抗瘧疾和抗炎劑。Chloroquinephosphate和toll-likereceptors(TLRs)的抑制劑。Chloroquinephosphate有效抑制SARS-CoV-2(COVID-19)感染(EC50=1.13μM)。IC50&TargetPlasmodiumMalariaTLRsSARS-COV-2HIV-1體外研究Chloroquine(CHQ,20μM)inhibitsIL-12p70releaseandreducesTh1-primingcapacityofactivatedhumanmonocyte-derivedLangerhans-likecells(MoLC).Chloroquine(CHQ,20μM)enhancesIL-1–inducedIL-23secretioninMoLCandsubsequentlyincreasesIL-17AreleasebyprimedCD4+Tcells[1].Chloroquine(25μM)suppressesMMP-9mRNAexpressioninnormoxiaandhypoxiainparentalMDA-MB-231cells.Chloroquinehascell-,dose-andhypoxia-dependenteffectsonMMP-2,MMP-9andMMP-13mRNAexpression[2].TLR7andTLR9inhibitionusingIRS-954orchloroquinesignificantlyreducesHuH7cellproliferationinvitro[3].Chloroquine(0.01-100μM;48?hours)potentlyblocksvirusinfection(veroE6cellsinfectedwithSARS-CoV-2)atlow-micromolarconcentration(EC50=?1.13?μM).ChloroquineblocksvirusinfectionbyincreasingendosomalpHrequiredforvirus/cellfusion,aswellasinterferingwiththeglycosylationofcellularreceptorsofSARS-CoV[4].體內研究Chloroquine(80mg/kg,i.p.)doesnotpreventthegrowthofthetriple-negativeMDA-MB-231cellswithhighorlowTLR9expressionlevelsintheorthotopicmousemodel[2].TLR7andTLR9inhibitionusingIRS-954orchloroquinesignificantlyinhibitstumourgrowthinthemousexenograftmodel.HCCdevelopmentintheDEN/NMORratmodelisalsosignificantlyinhibitedbychloroquine[3].PROTOCOLCellAssay[2]Thecellsareculturedin6-wellplateswithnormalculturemediuminthepresenceofvehicleor25or50μMchloroquine,untilnearconfluency,afterwhichtheyarerinsedwithsterilephosphate-bufferedsaline(PBS)andculturedfurtherfortheindicatedtimesinserum-freeculturemedium.Atthedesiredtime-points,theculturemediumisdiscardedandthecellsarequicklyharvestedinlysisbufferandclarifiedbycentrifugation.Subsequenttoboilingthesupernatantsinreducingsodiumdodecylsulphate(SDS)samplebuffer,equalamountsofprotein(100μg)areloadedperlaneandthesamplesareelectrophoresedinto10or4-20%gradientpolyacrylamideSDSgels,thentransferredtoanitrocellulosemembrane.TodetectTLR9,theblotsareincubatedovernightat4°Cwithanti-TLR9antibodies,diluted1:500inTris-bufferedsalinewith0.1%(v/v)Tween-20(TBST).Equalloadingisconfirmedwithpolyclonalrabbitanti-actin.Secondarydetectionisperformedwithhorseradishperoxidase-linkedsecondaryantibodies.TheproteinbandsarevisualizedbychemiluminescenceusinganECLkit.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalControlandTLR9siRNAMDA-MB-231cells(5×105cellsin100μL)areinoculatedintothemammaryfatAdministration[2]padsoffour-week-old,immune-deficientmice(athymicnude/nuFoxn1).Treatmentsarestartedsevendaysaftertumorcellinoculation.Themicearetreateddailyeitherwithintraperitoneal(i.p.)chloroquine(80mg/kg)orvehicle(PBS).Theanimalsaremonitoreddailyforclinicalsigns.TumormeasurementsareperformedtwiceaweekandtumorvolumeiscalculatedaccordingtotheformulaV=(π/6)(d1×d2)3/2,whered1andd2areperpendiculartumordiameters.Thetumorsareallowedtogrowfor22days,atwhichpointthemicearesacrificedandthetumorsaredissectedforafinalmeasurement.Throughouttheexperiments,theanimalsaremaintainedundercontrolledpathogen-freeenvironmentalconditions(20-21°C,30-60%relativehumidityanda12-hlightingcycle).Themicearefedwithsmall-animalfoodpelletsandsuppliedwithsterilewateradlibitum.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產品發(fā)表的科研?獻?NatBiotechnol.2022Jul25.?MolCancer.2019Apr10;18(1):85.?JInfection.2020Jun;80(6):e19-e26.?CircRes.2018May25;122(11):1532-1544.?JMedVirol.2022Oct10.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SaidA,etal.ChloroquinepromotesIL-17productionbyCD4+Tcellsviap38-dependentIL-23releasebymonocyte-derivedLangerhans-likecells.JImmunol.2014Dec15;193(12):6135-43.[2].TuomelaJ,etal.Chloroquinehastumor-inhibitoryandtumor-promotingeffectsintriple-negativebreastcancer.OncolLett.2013Dec;6(6):1665-1672.[3].MohamedFE,etal.Effectoftoll-likereceptor7and9targetedtherapytopreventthedevelopmentofhepatocellularcarcinoma.Liv