Pepstatin-Trifluoroacetate-Pepstatin-A-Trifluoroacetate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPepstatinTrifluoroacetateCat.No.:HY-P0018ASynonyms:PepstatinATrifluoroacetate分⼦式:C₃₆H₆₄F₃N₅O₁₁分⼦量:799.92Sequence:IsoValeryl-Val-Val-Sta-Ala-Sta-OHSequenceShortening:IsoVeryl-VV-Sta-A-Sta-OH作⽤靶点:HIVProtease;Autophagy作⽤通路:Anti-infection;MetabolicEnzyme/Protease;Autophagy储存⽅式:Sealedstorage,awayfrommoisturePowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:32mg/mL(40.00mM;Needwarming)H2O:1.1mg/mL(1.38mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.2501mL6.2506mL12.5013mL5mM0.2500mL1.2501mL2.5003mL10mM0.1250mL0.6251mL1.2501mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(2.60mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(2.60mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(2.60mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Pepstatin(PepstatinA)Trifluoroacetate由放线类产⽣的⼀种特异性的、具有⼝服活性的天冬氨酸蛋⽩酶(asparticproteases)抑制剂，能够抑制hemoglobin-pepsin、hemoglobin-proctase、casein-pepsin、casein-proctase、casein-acidprotease和hemoglobin-acidprotease的活性，IC50值分别为4.5nM、6.2nM、150nM、290nM、520nM和260nM；同时可抑制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]体外研究Pepstatin(PepstatinA)(7μM;48h)affectstheintracellularprocessingofHIV-specificgagprotein[2].体内研究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.户使⽤本产品发表的科研⽂献•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—您⾝边的抑制剂⼤师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