Octreotide-SMS-201-995-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEOctreotideCat.No.:HY-P0036CASNo.:83150-76-9Synonyms:SMS201-995分⼦式:C₄₉H₆₆N₁₀O₁₀S₂分⼦量:1019.24Sequence:Phe-Cys-Phe-Trp-Lys-Thr-Cys-Thr(Disulfidebridge:Cys2-Cys7)SequenceShortening:FCFWKTCT(Disulfidebridge:Cys2-Cys7)作⽤靶点:SomatostatinReceptor;Apoptosis作⽤通路:GPCR/GProtein;NeuronalSignaling;Apoptosis储存⽅式:ProtectfromlightPowder-80°C2years-20°C1year*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。BIOLOGICALACTIVITY⽣物活性Octreotide(SMS201-995)⼀种⽣长抑素受体(somatostatinreceptor)激动剂，合成⼋肽⽣长抑素类似物。Octreotide(SMS201-995)可与⽣长抑素受体(somatostatinreceptor)结合，主有2，3，5亚型，可增强Gi活性，降低胞内cAMP的产⽣。具有抗肿瘤活性，可介导细胞凋亡(apoptosis)，也可⽤于肢端肥⼤症的疾病研究。IC50&TargetSSTR2SSTR3SSTR5体外研究OctreotidereversesthePA-inducedalterationsinAktandGSK3βphosphorylationandexpressionofGSmRNAinHepG2cells[1].Octreotide(10‑8mM,6hours)inducesphosphorylated‑glycogensynthasekinase3β(GSK3β)phosphorylationandincreasesglycogensynthase(GS)activity[3].WesternBlotAnalysis[3]CellLine:HumanhepatoblastomaHepG2celllineConcentration:101/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE‑8mMIncubationTime:6hoursResult:Increasedtheproteinexpressionlevelsofphosphorylated‑AktandGSK3βby140.8%and12.2%,respectivelyandthemRNAlevelofGSalsoincreased.体内研究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].户使⽤本产品发表的科研⽂献•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