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

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

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CAS No. : 83150-76-9

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Based on 16 publication(s) in Google Scholar

Other Forms of Octreotide:

Top Publications Citing Use of Products

    Octreotide 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 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 21;14(1):962.  [Abstract]

    The efficacy of Octreotide acetate- and paltusotine-induced SSTR2 Gi signaling and β-arrestin recruitment.

    Octreotide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 21;14(1):962.  [Abstract]

    Internalization of SSTR2 in HEK293 cells treated with Octreotide acetate and paltusotine measured by ELISA assays by detecting the expression of SSTR2 on the cell surface. Data represent mean ± SEM from three independent experiments.

    Octreotide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 21;14(1):962.  [Abstract]

    eGFP-tagged SSTR2 plasmid was transfected in HEK293 cells and then cells were treated with Octreotide acetate (0-100 μM) for 30 min.

    Octreotide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 21;14(1):962.  [Abstract]

    Effects of mutations involved in Octreotide acetate binding of SSTR2 on Gi signaling.

    Octreotide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 21;14(1):962.  [Abstract]

    The effects of SSTR2 N2766.55A mutation on cAMP inhibition and β-arrestin recruitment induced by Octreotide acetate.

    Octreotide 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 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 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 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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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    SSTR2

     

    SSTR3

     

    SSTR5

     

    In Vitro

    Octreotide reverses the PA-induced alterations in Akt and GSK3β phosphorylation and expression of GS mRNA in HepG2 cells[1].
    Octreotide (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.
    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[1]. 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[2].

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

    Molecular Weight

    1019.24

    Formula

    C49H66N10O10S2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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)

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Sealed storage, away from moisture and light

    Powder -80°C 2 years
    -20°C 1 year

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 50 mg/mL (49.06 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.9811 mL 4.9056 mL 9.8112 mL
    5 mM 0.1962 mL 0.9811 mL 1.9622 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 100 mg/mL (98.11 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.96%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 0.9811 mL 4.9056 mL 9.8112 mL 24.5281 mL
    5 mM 0.1962 mL 0.9811 mL 1.9622 mL 4.9056 mL
    10 mM 0.0981 mL 0.4906 mL 0.9811 mL 2.4528 mL
    15 mM 0.0654 mL 0.3270 mL 0.6541 mL 1.6352 mL
    20 mM 0.0491 mL 0.2453 mL 0.4906 mL 1.2264 mL
    25 mM 0.0392 mL 0.1962 mL 0.3924 mL 0.9811 mL
    30 mM 0.0327 mL 0.1635 mL 0.3270 mL 0.8176 mL
    40 mM 0.0245 mL 0.1226 mL 0.2453 mL 0.6132 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • 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.

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    Product Name:
    Octreotide
    Cat. No.:
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