Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIslatravirCat.No.:HY-104012CASNo.:865363-93-5Synonyms:MK-8591分?式:C??H??FN?O?分?量:293.25作?靶點(diǎn):HIV;ReverseTranscriptase作?通路:Anti-infection儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(341.01mM;Needultrasonic)H2O:3.57mg/mL(12.17mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.4101mL17.0503mL34.1006mL5mM0.6820mL3.4101mL6.8201mL10mM0.3410mL1.7050mL3.4101mL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。-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)1/2MasterofBioactiveMolecules—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:≥2.08mg/mL(7.09mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.09mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.09mM);Clearsolution4.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥1.1mg/mL(3.75mM);Clearsolution5.請(qǐng)依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥1.1mg/mL(3.75mM);Clearsolution6.請(qǐng)依序添加每種溶劑：PBSSolubility:1.35mg/mL(4.60mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Islatravir(MK-8591)?種核苷逆轉(zhuǎn)錄酶(reversetranscriptase)抑制劑，具有抗HIV-1活性，對(duì)HIV-1(WT)，HIV-1(M184V)，HIV-1(MDR)的EC50值分別為0.068nM，3.1nM和0.15nM。IC50&TargetHIV-1(WT)HIV-1(MDR)HIV-1(M184V)0.068nM(EC50)0.15nM(EC50)3.1nM(EC50)體外研究Islatravir(MK-8591)(4'Ed2FA)isapotentanti-HIV-1agent,actingasanucleosidereversetranscriptaseinhibitor,withEC50sof0.068nM,3.1nMand0.15nMforHIV-1(WT),HIV-1(M184V),HIV-1(MDR),respectively[1].REFERENCES[1].OhruiH,etal.2'-deoxy-4'-C-ethynyl-2-fluoroadenosine,anucleosidereversetranscriptaseinhibitor,ishighlypotentagainstallhumanimmunodeficiencyvirusestype1andhaslowtoxicity.ChemRec.2006;6(3):133-43.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch