Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEIHVR-19029Cat.No.:HY-124662CASNo.:1447464-73-4分?式:C??H??N?O?分?量:443.62作?靶點:Glucosidase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:250mg/mL(563.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2542mL11.2709mL22.5418mL5mM0.4508mL2.2542mL4.5084mL10mM0.2254mL1.1271mL2.2542mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的?作液，建議您現?現配，當天使?；澄的儲備液可以根據儲存條件，適當保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥6.25mg/mL(14.09mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥6.25mg/mL(14.09mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥6.25mg/mL(14.09mM);Clearsolution1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性IHVR-19029?種有效的內質?α-葡萄糖苷酶Ⅰ和Ⅱ(α-glucosidasesI/II)抑制劑，對ERα-葡萄糖苷酶Ⅰ的IC50為0.48μM。IHVR-19029能有效阻斷?種出?熱病毒的復制，如登?病毒、埃博拉病毒和裂?熱病毒。IHVR-19029和Favipiravir(HY-14768)聯合提?抗病毒活性。體外研究IHVR-19029efficientlyinhibitsBovineviraldiarrheavirus(BVDV),Tacaribevirus(TCRV)andDenguevirus(DENV)withEC50sof0.25,0.74,and1.25μM,respectively[2].ThecombinationofIHVR-19029andFavipiravir(HY-14768)synergisticallyinhibitsthereplicationofYellowfeverandEbolavirusesinculturedcells[4].體內研究IHVR-19029(25-75mg/kg;I.p.;twicedailyfor10days)inhibitsEBOVandMARVinfectioninmice[2].IHVR-19029(5mg/kg;i.v.)hasAUC,C0,T1/2,CLandVdvaluesof1383μg*h/mL,1.79μg/mL,1.2hours,3.49L/h/kg,and3.0L/kg,respectively[2].IHVR-19029(75/5/5mg/kg;p.o./i.m./i.p.)hasAUCvaluesof945/1839/983μg*h/mL,Cmaxvaluesof0.26/1.23/1.33μg/ml,Tmaxvaluesof2.1/0.1/0.17hours,andFvaluesof4.6/71/133%,respectively[2].AnimalModel:BALB/cmice(12week233ofage)(MARVinfection)[2]Dosage:25,75mg/kgAdministration:I.p.;twicedaily,until10daysResult:SignificantprotectionofMarburgvirus(MARV)induceddeathwereobserved.AnimalModel:C57B1/6mice(8–12weekofage)(EBOVinfection)[2]Dosage:25,75mg/kgAdministration:I.p.;twicedailyfor10daysResult:Significantsurvivalwereobserved.REFERENCES[1].BrayM,etal.Meetingreport:31stInternationalConferenceonAntiviralResearch.AntiviralRes.2018Oct;158:88-102.

[2].ChangJ,etal.SmallmoleculeinhibitorsofERα-glucosidasesareactiveagainstmultiplehemorrhagicfeverviruses.AntiviralRes.2013;98(3):432‐440.[3].EsterProdrugsofIHVR-19029withEnhancedOralExposureandPreventionofGastrointestinalGlucosidaseInteraction.ACSMedChemLett.2017Jan17;8(2):157-162.[4].MaJ,etal.EnhancingtheantiviralpotencyofERα-glucosidaseinhibitorIHVR-19029againsthemorrhagicfevervirusesinvitroandinvivo.AntiviralRes.2018Feb;150:112-122.McePdfHeight2/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvali