Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEOctreotideCat.No.:HY-P0036CASNo.:83150-76-9Synonyms:SMS201-995分?式:C??H??N??O??S?分?量:1019.24Sequence:Phe-Cys-Phe-Trp-Lys-Thr-Cys-Thr(Disulfidebridge:Cys2-Cys7)SequenceShortening:FCFWKTCT(Disulfidebridge:Cys2-Cys7)作?靶點(diǎn):SomatostatinReceptor;Apoptosis作?通路:GPCR/GProtein;NeuronalSignaling;Apoptosis儲存?式:ProtectfromlightPowder-80°C2years-20°C1year*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。BIOLOGICALACTIVITY?物活性O(shè)ctreotide(SMS201-995)?種?長抑素受體(somatostatinreceptor)激動劑，合成?肽?長抑素類似物。Octreotide(SMS201-995)可與?長抑素受體(somatostatinreceptor)結(jié)合，主有2，3，5亞型，可增強(qiáng)Gi活性，降低胞內(nèi)cAMP的產(chǎn)?。具有抗腫瘤活性，可介導(dǎo)細(xì)胞凋亡(apoptosis)，也可?于肢端肥?癥的疾病研究。IC50&TargetSSTR2SSTR3SSTR5體外研究OctreotidereversesthePA-inducedalterationsinAktandGSK3βphosphorylationandexpressionofGSmRNAinHepG2cells[1].Octreotide(10?8mM,6hours)inducesphosphorylated?glycogensynthasekinase3β(GSK3β)phosphorylationandincreasesglycogensynthase(GS)activity[3].WesternBlotAnalysis[3]CellLine:HumanhepatoblastomaHepG2celllineConcentration:101/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?8mMIncubationTime:6hoursResult:Increasedtheproteinexpressionlevelsofphosphorylated?AktandGSK3βby140.8%and12.2%,respectivelyandthemRNAlevelofGSalsoincreased.體內(nèi)研究OctreotidesignificantlylowerstheplasmaglucoselevelsintheobeseratsoftheHFDgroup.Octreotideinterventionsignificantlydecreasestheseruminsulinconcentration;however,thereisnomarkedreductioninserumTG,TC,FFA,ALTandASTlevels.OctreotidesignificantlyinhibitstheHOMAindex.OctreotidedecreasesipGTTandipITTAUCs,butnotsignificantly.OctreotideimprovesfatdegenerationinratswithHFD-inducedobesityandlipiddropletaccumulationinPA-treatedHepG2cells.OctreotidepromotesthephosphorylationofAktandGSK3βandtheexpressionofGSmRNAinratswithHFD-inducedobesity[1].Octreotidereducesbodyweightandwetkidneyweightcomparedwiththevehicle-treated(CONT)group.PASandOctreotide/PAStreatmentdecreasecAMPlevels,butOctreotidealonedoesnotinPCKrats.IntheOctreotide/PASgroup,thereareasignificantlyfewerpS6-positivecellsthaninthePASalonegroup[2].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JPharmSci.2022Oct10;S0022-3549(22)00454-3.?BasicClinPharmacolToxicol.2022Jun10.?JPharmBiomedAnal.2022:115156.?JPharmBiomedAnal.11December2021,114518.?ResearchSquarePrint.2022Aug.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Xiao-XiaWang,etal.Effectsofoctreotideonhepaticglycogenesisinratswithhighfatdiet?inducedobesity.MolMedRep.2017Jul;16(1):109-118.[2].WangXX,etal.Effectsofoctreotideonhepaticglycogenesisinratswithhighfatdiet?inducedobesity.MolMedRep.2017Jul;16(1):109-118[3].KugitaM,etal.BeneficialeffectofcombinedtreatmentwithoctreotideandpasireotideinPCKrats,anorthologousmodelofhumanautosomalrecessivepolycystickidneydisease.PLoSOne.2017May18;12(5):e0177934.McePdfHeightCaution:Producthasnotbeenfullyvalidate