2. GPCR/G Protein Neuronal Signaling Apoptosis
  3. Somatostatin Receptor Apoptosis
  4. Octreotide pamoate

Octreotide pamoate  (Synonyms: SMS 201-995 pamoate)

目录号: HY-P0036B
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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。

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Custom Peptide Synthesis

Octreotide pamoate

Octreotide pamoate Chemical Structure

CAS No. : 135467-16-2

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Octreotide pamoate 的其他形式现货产品:

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Octreotide pamoate 相关抗体

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查看 Somatostatin Receptor 亚型特异性产品:

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SSTR1 SSTR2 SSTR3 SSTR5 SSTR4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly[1][2].

IC50 & Target

SSTR2

 

SSTR3

 

SSTR5

 

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Octreotide pamoate 相关抗体:

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Formula

C49H66N10O10S2.xC23H16O6
CAS 号
Sequence

{d-Phe}-Cys-Phe-{d-Trp}-Lys-Thr-Cys-{d-Threoninol} (Disulfide bridge: Cys2-Cys7)
Sequence Shortening

{d-Phe}-CF{d-Trp}-KTC-{d-Threoninol} (Disulfide bridge: Cys2-Cys7)
中文名称

双羟萘酸奥曲肽
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.
纯度 & 产品资料
参考文献

Octreotide pamoate 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Octreotide135467-16-2SMS 201-995双羟萘酸奥曲肽Somatostatin ReceptorApoptosisSSTRsSSTRSomatostatin receptor agonistAcromegalyCancerInhibitorinhibitorinhibit

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