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Octreotide

CAS No. : 83150-76-9

MCE 国际站：Octreotide

产品活性：Octreotide (SMS 201-995) 是一种生长抑素受体 (somatostatin receptor) 激动剂，合成八肽生长抑素类似物。Octreotide (SMS 201-995) 可与生长抑素受体 (somatostatin receptor) 结合，主要有 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。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Apoptosis

作用靶点：Somatostatin Receptor  |  Apoptosis

In Vitro: Octreotide reverses the PA-induced alterations in Akt and GSK3β phosphorylation and expression of GS mRNA in HepG2 cells.
Octreotide (10 ⁸mM, 6 hours) induces phosphorylated glycogen synthase kinase 3β (GSK3β) phosphorylation and increases glycogen synthase (GS) activity.

In Vivo: Octreotide significantly lowers the plasma glucose levels in the obese rats of the HFD group. Octreotide intervention significantly decreases the serum insulin concentration; however, there is no marked reduction in serum TG, TC, FFA, ALT and AST levels. Octreotide significantly inhibits the HOMA index. Octreotide decreases ipGTT and ipITT AUCs, but not significantly. Octreotide improves fat degeneration in rats with HFD-induced obesity and lipid droplet accumulation in PA-treated HepG2 cells. Octreotide promotes the phosphorylation of Akt and GSK3β and the expression of GS mRNA in rats with HFD-induced obesity. Octreotide reduces body weight and wet kidney weight compared with the vehicle-treated (CONT) group. PAS and Octreotide/PAS treatment decrease cAMP levels, but Octreotide alone does not in PCK rats. In the Octreotide/PAS group, there are a significantly fewer pS6-positive cells than in the PAS alone group.

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