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

Octreotide pamoate  (Synonyms: SMS 201-995 pamoate)

製品番号: HY-P0036B
取扱説明書 Technical Support

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.

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カスタムペプチド

CAS 番号 : 135467-16-2

容量 在庫状況
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Other 在庫あり Forms of Octreotide pamoate:

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Top Publications Citing Use of Products

    Octreotide pamoate purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 20;23(1):205.  [Abstract]

    In vivo assessment of octreotide sensitivity in GH3 xenografts by injecting with or without Fto knockdown GH3 cells according to tumor volume, tumor weight and growth hormone level. Octreotide (OCT) (50 μg/kg; i.p.; once daily) inhibited the growth of FTO-knockdown cells effectively and further reduced the secretion of growth hormone.

    Octreotide pamoate purchased from MedChemExpress. Usage Cited in: Basic Clin Pharmacol Toxicol. 2022 Sep;131(3):174-188.  [Abstract]

    Effects of 0ctreotide (10 μM; 4, 8, 24 and 48 h) on cell viability after treatments. 0ctreotide significantly inhibited 3T3-L1 cell viability after 8, 24 and 48 h but not 4 h.

    Octreotide pamoate purchased from MedChemExpress. Usage Cited in: Basic Clin Pharmacol Toxicol. 2022 Sep;131(3):174-188.  [Abstract]

    Representative western blot brands of PI3K, Akt and p-Akt with or without Octreotide (2.5-10 μM) treatments. Octreotide suppressed the expression of PI3K and p-Akt in a dose-dependent manner but showed no effects on the total Akt expression in 3T3-L1 cells.

    Octreotide pamoate purchased from MedChemExpress. Usage Cited in: Basic Clin Pharmacol Toxicol. 2022 Sep;131(3):174-188.  [Abstract]

    Oil Red O staining was performed to illustrate lipid droplets and to determine the lipid contents. Octreotide (2.5-10 μM) treatments significantly reduced lipid contents in 3T3-L1 cells on Day 6 and Day 12 compared with the control.

    Octreotide pamoate purchased from MedChemExpress. Usage Cited in: Basic Clin Pharmacol Toxicol. 2022 Sep;131(3):174-188.  [Abstract]

    mRNA expression of Pparg, Cebpa, Fasn, and Fabp4 with or without Octreotide (2.5–10 μM; 12 d) treatments. Octreotide suppressed mRNA levels of Pparg, Cebpa, Fasn, and Fabp4 in 3T3-L1 preadipocytes in a dose-dependent manner.

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    製品説明

    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

     

    体外実験

    Octreotide pamoate (10 8mM, 6 hours) induces phosphorylated glycogen synthase kinase 3β (GSK3β) phosphorylation and increases glycogen synthase (GS) activity[3].

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

    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.
    体内実験

    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].

    MedChemExpress (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.
    分子式

    C49H66N10O10S2.xC23H16O6

    CAS 番号
    Sequence

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

    Sequence Shortening

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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    Please store the product under the recommended conditions in the Certificate of Analysis.

    純度とドキュメンテーション
    参考文献
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      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.

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    製品名:
    Octreotide pamoate
    製品番号:
    HY-P0036B
    数量:
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