Octreotide (SMS 201-995) pamoate 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 pamoate 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。
| 生物活性 | Octreotide (SMS 201-995) pamoate is asomatostatin receptoragonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to thesomatostatin receptorswhich are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediatesapoptosisand may also be used in disease studies in acromegaly[1][2]. |
体外研究
(In Vitro) | Octreotide pamoate (10-8mM, 6 hours) induces phosphorylated-glycogen synthase kinase 3β (GSK3β) phosphorylation and increases glycogen synthase (GS) activity[3].
Western Blot Analysis[3] | Cell Line: | Human hepatoblastoma HepG2 cell line | | Concentration: | 10-8mM | | Incubation Time: | 6 hours | | Result: | Increased the protein expression levels of phosphorylated-Akt and GSK3β by 140.8% and 12.2%, respectively and the mRNA level of GS also increased. |
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体内研究
(In Vivo) | Octreotide pamoate (subcutaneous injection, 30 mg/kg, once) can inhibit tumor growth significantly with no effect on body weight[1].
Octreotide pamoate (intramuscular injection, 60 mg/kg, every 21 days, 42 days) inhibits serum insulin-like growth factor (IGF-I) without toxicity in dogs with appendicular osteosarcoma (OSA)[2].
Octreotide pamoate (subcutaneous injection, 40 μg/kg, Every 12 hours, 8 days) improves hepatic glycogen synthesis in obese male Sprague-Dawley (SD) rats[3].
| Animal Model: | Female nude mice (nu/nu Balbc-A weighing 19-22 g)[1] | | Dosage: | 30 mg/kg | | Administration: | Subcutaneous injection; once | | Result: | Showed that the average volume of tumors treated was 25.8% of the control group and no effect on body weight. |
| Animal Model: | Dogs with appendicular OSA[2] | | Dosage: | 60 mg/kg | | Administration: | Intramuscular injection; every 21 days; 42 days | | Result: | Resulted in a 43% decrease in mean serum IGF-I compared with mean baseline concentrations. |
| Animal Model: | Male Sprague-Dawley (SD) rats (3 weeks; 40-60 g)[3] | | Dosage: | 40 μg/kg | | Administration: | Subcutaneous injection; every 12 hours; 8 days | | Result: | Significantly improved fat deposition and reduced lipid infiltration. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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