Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPepstatinTrifluoroacetateCat.No.:HY-P0018ASynonyms:PepstatinATrifluoroacetate分?式:C??H??F?N?O??分?量:799.92Sequence:IsoValeryl-Val-Val-Sta-Ala-Sta-OHSequenceShortening:IsoVeryl-VV-Sta-A-Sta-OH作?靶點:HIVProtease;Autophagy作?通路:Anti-infection;MetabolicEnzyme/Protease;Autophagy儲存?式:Sealedstorage,awayfrommoisturePowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:32mg/mL(40.00mM;Needwarming)H2O:1.1mg/mL(1.38mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.2501mL6.2506mL12.5013mL5mM0.2500mL1.2501mL2.5003mL10mM0.1250mL0.6251mL1.2501mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?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：1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(2.60mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(2.60mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(2.60mM);ClearsolutionBIOLOGICALACTIVITY?物活性Pepstatin(PepstatinA)Trifluoroacetate由放線類產(chǎn)?的?種特異性的、具有?服活性的天冬氨酸蛋?酶(asparticproteases)抑制劑，能夠抑制hemoglobin-pepsin、hemoglobin-proctase、casein-pepsin、casein-proctase、casein-acidprotease和hemoglobin-acidprotease的活性，IC50值分別為4.5nM、6.2nM、150nM、290nM、520nM和260nM；同時可抑制HIVprotease的活性。IC50&TargetIC50:4.5nM(Hemoglobin-pepsin),6.2nM(Hemoglobin-proctase),150nM(Casein-pepsin),260nM(Hemoglobin-acidprotease),290nM(Casein-proctase),520nM(Casein-acidprotease)[1]體外研究Pepstatin(PepstatinA)(7μM;48h)affectstheintracellularprocessingofHIV-specificgagprotein[2].體內(nèi)研究Pepstatin(PepstatinA)hasaverylowtoxicity,withLD50sof1090mg/kg,875mg/kg,820mg/kgand450mg/kgformice,rats,rabbits,anddogsbyi.p.route,and>2000mg/kgforallspeciesbyoralroute[1].Pepstatin(0.5-50mg/kg,p.o.)suppressesstomachulcerationofthepylorusinligatedShayrats[1].AnimalModel:PylorusligatedmaleWistarrats[1]Dosage:0.5,1,10and50mg/kgAdministration:Oraladministration,15minutesafterpyloricligationResult:Effectivelypreventedstomachulceration.戶使?本產(chǎn)品發(fā)表的科研?獻?AdvSci(Weinh).2022Oct10;e2203831.?IntJAntimicrobAgents.2019Dec;54(6):814-819.?SciAdv.2022Nov11;8(45):eabn6579.?EnvironSciTechnol.2017Dec5;51(23):13938-13948.?PharmacolRes.2021Dec1;175:105985.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].UmezawaH,etal.Pepstatin,anewpepsininhibitorproducedbyActinomycetes.JAntibiot(Tokyo).1970May;23(5):259-62.[2].SeelmeierS,etal.Humanimmunodeficiencyvirushasanaspartic-typeproteasethatcanbeinhibitedbypepstatinA.ProcNatlAcadSciUSA.1988Sep;85(18):6612-6.McePdfHeightCaution:Producthasnotbeenfully