Tetragastrin-Cholecystokinin-tetrapeptide-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETetragastrinCat.No.:HY-125556CASNo.:1947-37-1Synonyms:Cholecystokinintetrapeptide;CCK-4分⼦式:C₂₉H₃₆N₆O₆S分⼦量:596.7SequenceShortening:WMDF-NH2作⽤靶点:CholecystokininReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Sealedstorage,awayfrommoisturePowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(83.79mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6759mL8.3794mL16.7588mL5mM0.3352mL1.6759mL3.3518mL10mM0.1676mL0.8379mL1.6759mL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：(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1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE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:≥2.5mg/mL(4.19mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.19mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.19mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Tetragastrin(Cholecystokinintetrapeptide;CCK-4)胃泌素的C-末端四肽，能刺激胃液分泌。Tetragastrin⼀种胆囊收缩素(CCK-4)受体激动剂。Tetragastrin具有胃黏膜保护。体外研究TheantagonistofhistamineH2-receptors,CimetidineinhibitsthestimulatoryeffectofhistamineinvitroandactivatesTetragastrinstimulationoftheadenylatecyclaseactivity.Tetragastrinandhistamineactivateadenylatecyclaseoftheratgastricmucosaviadifferentreceptors[4].体内研究IninbredWistarratstreatedwithN-methyl-N'-nitro-N-nitrosoguanidine,Tetragastrin(s.c.;1mg/kg;everyotherday)treatmentsignificantlyreducestheincidenceandthenumberofadenocarcinomas,andhasasignificantlylowerlabellingindexoftheantralmucosa[1].Tetragastrinhaspotentialforenhancinggastricmucosalprotectionassociatedwithmucussecretionand/ormucussynthesisonthesurfacemucosaofratgastricmucosa.Asignificantincreaseinthemucincontentwasnotedinthemucusgelandsurfacemucosallayer.AnincreaseinmucininthemucusgelandsurfacemucosawouldthusappearduetotheadministrationofTetragastrin[3].AnimalModel:Seven-week-oldmaleWistarrats,eachweighingapproximately160g[3]Dosage:12,120,or400μg/kgAdministration:Administeredsubcutaneously(s.c.);followedby50%ethanol-inducedgastricinjuryResult:Causedasignificantincreaseinmucincontentinthecorpusmucosaandprevented50%ethanol-inducedgastricmucosaldamageinadose-dependentmanner.REFERENCES[1].MTatsuta,etal.Effectof6-hydroxydopamineongastriccarcinogenesisandtetragastrininhibitionofgastriccarcinogenesisinducedbyN-methyl-N'-nitro-N-nitrosoguanidineinWistarrats.CancerRes.1989Aug1;49(15):4199-203.[2].AAKarelin,etal.Tetragastrinactivationofratgastricmucosaadenylcyclaseinvitro.BiullEkspBiolMed.1981Apr;91(4):440-1.[3].NathalieLara,etal.PulmonaryandsystemicnitricoxidemeasurementsduringCCK-5-inducedpanicattacks.Neuropsychopharmacology.2003Oct;28(10):1840-5.[4].YKomuro,etal.Effectsoftetragastrinonmucusglycoproteininratgastricmucosalprotection.GastroenterolJpn.1992Oct;27(5):597-2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE603.McePdfHeightCaution:Producthas