Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERetro-2Cat.No.:HY-122571CASNo.:1201652-50-7分?式:C??H??N?OS分?量:320.41作?靶點(diǎn):Filovirus;Parasite;Autophagy作?通路:Anti-infection;Autophagy儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(780.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.1210mL15.6050mL31.2100mL5mM0.6242mL3.1210mL6.2420mL10mM0.3121mL1.5605mL3.1210mL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(protectfromlight)。-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.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(6.49mM);Suspendedsolution;Needultrasonic2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(6.49mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.49mM);ClearsolutionBIOLOGICALACTIVITY?物活性Retro-2?種內(nèi)體蛋?質(zhì)-?爾體逆?運(yùn)輸?shù)倪x擇性抑制劑。Retro-2?種埃博拉病毒(EBOV)感染抑制劑，在HeLa細(xì)胞中的EC50為12.2μM。Retro-2還可誘導(dǎo)細(xì)胞?噬(autophagy)。IC50&TargetEC50:12.2μM(Ebolavirus)[3]體外研究Retro-2(1μM;1-4hours)inducesautophagyinGFP-LC3-expressingHeLacellsandpromotedthedramaticcytoplasmicaccumulationoflargeautophagosomes[2].Retro-2(1μM;0.5-4hours)treatmenthowsanincreaseovertimeoftheabundanceofLC3-IIproteinincells[2].Retro-2impairsthetraffickingbetweenautophagosomesandlysosomes.Retro-2abolishesautolysosomesformation[2].Retro-2(20μM;pretreatmentfor30min)inhibitsHeLacellintoxicationbyricin,Shiga-liketoxins1(Stx1)and2(Stx2)[1].Retro-2blockedinvasionofcellsbytheintracellularparasiteLeishmania,aswellasreplicationofnon-envelopedviruses,includingpolyoma-,papilloma-,andadeno-associatedviruses[3].CellAutophagyAssay[2]CellLine:HeLacellsConcentration:1μMIncubationTime:1hour,2hours,4hoursResult:Resultedinalargesignificantincreaseinthenumberofsmallandlargevesicles.WesternBlotAnalysis[2]CellLine:HeLacellsConcentration:1μMIncubationTime:0.5hour,2hours,4hoursResult:ShowedanincreaseovertimeoftheabundanceofLC3-IIproteinincells.體內(nèi)研究Retro-2(2-200mg/kg;i.p;daily;for21days)treatmentclearlyprotectsfromlethalnasalexposuretoricininmice.200mg/kgofRetro-2fullyprotectsmiceagainstricinchallenge[1].AnimalModel:FemaleBalb/cmice(Pathogen-free6-week-old)injectedwithricin(2μg/kg)[1]2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:2mg/kg,10mg/kg,20mg/kg,200mg/kgAdministration:Intraperitonealinjection;daily;for21daysResult:Protectedmiceagainstricinchallenge.REFERENCES[1].BahneStechmann,etal.Inhibitionofretrogradetransportprotectsmicefromlethalricinchallenge.Cell.2010Apr16;141(2):231-42.[2].ValérieNicolas,etal.SmallTraffickingInhibitorRetro-2DisruptstheMicrotubule-DependentTraffickingofAutophagicVacuoles.FrontCellDevBiol.2020Jun18;8:464.[3].OlenaShtanko,etal.Retro-2anditsdihydroquinazolinonederivativesinhibitfilovirusinfection.AntiviralRes.2018Jan;149:154-163.McePdfHeightCaution:Producthasno