Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECeruletideCat.No.:HY-A0190CASNo.:17650-98-5Synonyms:Caerulein;Cerulein;FI-6934分?式:C??H??N??O??S?分?量:1352.41Sequence:{pGlu}-Gln-Asp-Tyr(SO3H)-Thr-Gly-Trp-Met-Asp-Phe-NH2SequenceShortening:{pGlu}-QD-Y(SO3H)-TGWMDF-NH2作?靶點:CholecystokininReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY?物活性Ceruletide?種?肽，也?種有效的膽囊收縮素受體(cholecystokininreceptor)激動劑。Ceruletide是?種安全有效的膽囊收縮劑，對膽囊肌?和膽管有直接的痙攣性作?。IC50&TargetCholecystokininreceptor[4]體外研究Ceruletideissimilarchemicallyandbiologicallytothehumangastrointestinalhormonescholecystokinin-pancreozymin(CCK)andgastrinII.Ceruletidestimulatesgallbladdercontraction,pancreaticexocrinesecretion,gastricsecretion,andmotilityinthedistalduodenum,jejunum,ileumandcolon,whiledelayinggastricemptyingandinhibitingmotilityintheproximalduodenum[1].CeruletideinsupramaximalbutnotinphysiologicaldosesactivatesNF-kappaB/Relinvitro.Thisactivationmayinduceaself-defendinggeneticprogrambeforetheonsetofcellularinjury,whichmaypreventhigherdegreesofdamageofpancreaticacinarcellsaftersecretagoguehyperstimulation[2].體內(nèi)研究Ceruletide(0.4-0.5mcg/kg,i.v.;3-4mcg/kg,s.c.)resultsinemesisandevacuationofthebowelintheintactconsciousdog,andrecoveryiscomplete15-30minafteri.v.administrationand2-4hrafters.c.administration.Ceruletide(5-15ng/kg,i.v.)showsamarkedspasmogeniceffectonthepylorusofrats.1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECeruletidealsoreducesbloodpressureinanesthetizeddogs[1].Ceruletideserumbileacid(SBA)stimulationcircumventsexogenousandendogenousinfluencesassociatedwithpostprandial(PP)SBAstimulation.CeruletideSBAstimulationmayperformaswellasPPSBAstimulationindogswithportosystemicshunt(PSS)andbemoresensitiveforthedetectionofhepaticdysfunctionindogswithupperrespiratorydisease(URD)[3].PROTOCOLAnimalDogs[3]Administration[3]Alldogsundergoserumbileacid(SBA)stimulationwithfood(5kgBW2tablespoons)or0.3μg/kgBWCeruletideIM,respectively,onconsecutivedays.Adietofmoderateproteincontentandwithanincreasedconcentrationoffiberischosentominimizemetaboliccomplicationssuchashepaticencephalopathy.Beforeeachtest,thedogsarefastedfor12hours.Bloodsamplesaredrawnatbaseline,60and120minutesafterfeeding,and20,30,and40minutespostinjection,respectively.Thebloodsamplesarecollectedinplaintubesandlefttoclot;theyarethencentrifugedat6,500×gfor1minute,andtheserumisusedtomeasureSBAbyacolorimetrictestwithendpointdetermination[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻?ChemEngJ.15October2022,136792.?SciAdv.2020Aug5;6(32):eaba8415.?JExpClinCancerRes.2021Jan9;40(1):25.?CellDeathDis.2021Oct11;12(10):928.?CellDeathDis.2021Mar15;12(3):273.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].VincentME,etal.Pharmacology,clinicaluses,andadverseeffectsofceruletide,acholecystokineticagent.Pharmacotherapy.1982Jul-Aug;2(4):223-34.[2].SteinleAU,etal.NF-kappaB/Relactivationinceruleinpancreatitis.Gastroenterology.1999Feb;116(2):420-30.[3].BridgerN,etal.Comparisonofpostprandialandceruletideserumbileacidstimulationindogs.JVetInternMed.2008Jul-Aug;22(4):873-8.[4].ZarrindastMR,etal.Effectsofcholecystokininreceptoragonistandantagonistsonmorphindependenceinmice.PharmacolToxicol.1995Dec;77(6):360-4.McePdfHeightCaution: