Lufotrelvir-PF-07304814-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELufotrelvirCat.No.:HY-138078CASNo.:2468015-78-1Synonyms:PF-07304814分?式:C??H??N?O?P分?量:552.51作?靶點:SARS-CoV作?通路:Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據體外實驗DMSO:130mg/mL(235.29mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8099mL9.0496mL18.0992mL5mM0.3620mL1.8099mL3.6198mL10mM0.1810mL0.9050mL1.8099mL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；?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。-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：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥3.25mg/mL(5.88mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥3.25mg/mL(5.88mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:3.25mg/mL(5.88mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Lufotrelvir(PF-07304814)PF-00835231的磷酸前藥，?種有效的3CLpro蛋?酶(Mpro)抑制劑，具有SARS-CoV-2抗病毒活性。Lufotrelvir結合并抑制SARS-CoV-23CLpro活性，Ki為174nM。Lufotrelvir?種很有前途的單?抗病毒試劑，也可?于與針對冠狀病毒?命周期其他關鍵階段的其他抗病毒試劑的聯(lián)合研究。體內研究Onceadministeredthroughintravenousinfusion,LufotrelviriscleavedintoPF-00835231toexertitsanti-viraleffects.Lufotrelvirexhibitsafavorablecardiovascularsafetyprofile[1].Lufotrelvirisadministeredintravenouslytorats,dogsandmonkeys.Itexhibitshighsystemicclearanceandshorthalf-lifeacrossspeciesforming68,81,76%PF-00835231inrats,dogsandmonkeyrespectivelyincomparisontothesystemicexposureachievedwithIVadministrationofPF00835231[1].REFERENCES[1].KoenVandyck,etal.Considerationsforthediscoveryanddevelopmentof3-chymotrypsin-likecysteineproteaseinhibitorstargetingSARS-CoV-2infection.CurrOpinVirol.2021Apr27;49:36-40.[2].BrittonBoras,etal.Title:DiscoveryofaNovelInhibitorofCoronavirus3CLProteaseasaClinicalCandidateforthePotentialTreatmentofCOVID-19ShortTitle:Novel3CLProteaseInhibitorforCOVID-19McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc