Daclatasvir-dihydrochloride-BMS-790052-dihydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDaclatasvirdihydrochlorideCat.No.:HY-10465CASNo.:1009119-65-6Synonyms:BMS-790052dihydrochloride;EBP883dihydrochloride分?式:C??H??Cl?N?O?分?量:811.8作?靶點(diǎn):HCV作?通路:Anti-infection儲(chǔ)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:≥56mg/mL(68.98mM)H2O:50mg/mL(61.59mM;Needultrasonic)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.2318mL6.1592mL12.3183mL5mM0.2464mL1.2318mL2.4637mL10mM0.1232mL0.6159mL1.2318mL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；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1mg/mL(1.23mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1mg/mL(1.23mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1mg/mL(1.23mM);ClearsolutionBIOLOGICALACTIVITY?物活性Daclatasvirdihydrochloride(BMS-790052dihydrochloride)?種有效的具有?服活性的HCVNS5A蛋?抑制劑，多種HCV復(fù)制?因型的EC50范為9-146pM。Daclatasvirdihydrochloride也有機(jī)離?轉(zhuǎn)運(yùn)多肽1B(OATP1B)和OATP1B3抑制劑，IC50分別為1.5μM和3.27μM。IC50&TargetEC50:50pM(HCVreplicongenotype1a),9?pM(HCVreplicongenotype1b),71pM(HCVreplicongenotype2a),146pM(HCVreplicongenotype3a),12pM(HCVreplicongenotype4a)and33pM(HCVreplicongenotype5a)[1]Kd:8nM(NS5A33-202)and210nM(NS5A26-202)[2]IC50:1.5μM(OATP1B)and3.27μM(OATP1B3)[3]體外研究Daclatasvir(BMS-790052)demonstratespotentinhibitoryactivitytowardsallgenotypestested,withEC50valuesrangingfrom9pMto146?pM.DaclatasvirinhibitsHCVreplicongenotype1a,1b,2a,3a,4aand5awithEC50valuesof50pM,9?pM,71pM,146pM,12pMand33pM,respectively.DaclatasvirisapotentinhibitoroftheJFH-1genotype2ainfectiousvirusthatreplicatesincellculture(EC50=28pM)[1].Daclatasvir(BMS-790052)bindstightlytoNS5A33-202andNS5A26-202withKdsof8nMand210nM,respectively[2].體內(nèi)研究Daclatasvir(BMS-790052;30?mg/kg;oraladministration;daily;for27days)treatmentreducesserumHCVRNAtitersveryrapidlyby~1.5log10atday3[4].AnimalModel:NOD/SCIDmalemice(5weeksofage,18-20?g)bearingHCVRNA-transfectedcells[4]Dosage:30?mg/kgAdministration:Oraladministration;daily;for27daysResult:ReducedserumHCVRNAtitersveryrapidlyby~1.5log10atday3.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Hepatology.2019May;69(5):1861-1872.?IntJAntimicrobAgents.2015Oct;46(4):381-8.?AntiviralRes.2020May;177:104734.?AntiviralRes.2017Dec;148:5-14.?AntiviralRes.2017Oct;146:191-200.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].MinGao,etal.ChemicalgeneticsstrategyidentifiesanHCVNS5Ainhibitorwithapotentclinicaleffect.Nature.2010May6;465(7294):96-100.[2].DavidBAscher,etal.PotenthepatitisCinhibitorsbinddirectlytoNS5AandreduceitsaffinityforRNA.SciRep.2014Apr23;4:4765.[3].TomomiFurihata,etal.Differentinteractionprofilesofdirect-actinganti-hepatitisCvirusagentswithhumanorganicaniontransportingpolypeptides.AntimicrobAgentsChemother.2014Aug;58(8):4555-64.[4].Seung-HoonLee,etal.HA1077displayssynergisticactivitywithdaclatasviragainsthepatitisCvirusandsuppressestheemergenceofNS5Aresistance-associatedsubstitutionsinmice.SciRep.2018Aug20;8(1):12469.McePdfHeightCa