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

Octreotide acetate  (Synonyms: SMS 201-995 acetate)

Cat. No.: HY-17365 Purity: 99.92%
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SDS
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Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

CAS No. : 79517-01-4

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Octreotide acetate:

Octreotide acetate Related Antibodies

Top Publications Citing Use of Products

    Octreotide acetate 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 acetate 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 acetate 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 acetate 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 acetate 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 acetate 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 acetate 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 acetate 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 acetate 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 acetate 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

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

    In Vivo

    Octreotide-treated groups show a significant reduction in the tumor volume when compared with saline group. Octreotide-PPSG (1.4 mg/kg, i.p.) shows greater antitumor effect than Octreotide-soln (100 μg/kg, i.p.). Octreotide-treatments results in significant inhibitory effect on the expression levels of SSTR2 and SSTR5 in primary HCC-bearing rats compared with the saline group. Octreotide-PPSG appears to inhibit the expression of SSTR2 and SSTR5 to a greater extent than that of Octreotide-soln treated group[1]. A test dose of octreotide acetate significantly decreases the serum gastrin level to approximately one third of the baseline in 2 hr and the effect lasted approximately for 6 hr. On day 21, treatment with sustained-release formulation of octreotide acetatea (5 mg intramuscular, q 4 wk) is initiated[2].

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

    1079.29

    Formula

    C51H70N10O12S2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    Sequence

    {d-Phe}-Cys-Phe-{d-Trp}-Lys-Thr-{Cys(X)}-{Thr(deoxy)} (disulfide bridge: Cys2-Cys7) (X=N-(1R,2R)-2-hydroxy-1-(hydroxymethyl)propyl)
    Sequence Shortening

    {d-Phe}-CF-{d-Trp}-KY-{Cys(X)}-{Thr(deoxy)} (disulfide bridge: Cys2-Cys7) (X=N-(1R,2R)-2-hydroxy-1-(hydroxymethyl)propyl)
    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

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (92.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 25 mg/mL (23.16 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.9265 mL 4.6327 mL 9.2654 mL
    5 mM 0.1853 mL 0.9265 mL 1.8531 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.25 mg/mL (2.08 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.25 mg/mL (2.08 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    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 (92.65 mM); Clear solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    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: 99.93%

    SDS (393 KB)

    COA (263 KB) HNMR (323 KB) LCMS (91 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    Mice[1]
    Thirty mice with HCC xenografts are randomLy divided into three groups: (A) Octreotide-soln group, (B) Octreotide-PPSG group, and (C) control group. Octreotide-soln group receives i.p. injection of 100 μg/kg octreotide-soln once a day and totally for consecutive 14 days. Octreotide-PPSG group receives a single subcutaneous injection of 1.4 mg/kg Octreotide-PPSG, and the injection volume is about 0.2 mL. Control group receives i.p. injection of saline once a day for consecutive 14 days. Treatment starts on the next day after injection of H22 hepatoma cell suspension and maintains for 14 days. Tumor growth is monitored by periodic caliper measurements on day 7 and day 14 post seeding. Tumor volumes (V) are calculated based on the length and width of tumor by Eq.
    Rats[1]
    Twelve male SD rats are divided into two groups, and housed in standard cages at 25°C, with free access to food and water for a week prior to the experiment. Rats are subcutaneously injected with Octreotidereotide solution (Octreotide-soln) or Octreotide-PPSG at an equivalent single dose of 20 mg/kg. The dose is determined based on the clinical dose of Octreotide-soln in human. Rats are fasted for 12 h before dosing and food is returned approximately 2 h post dosing. Blood samples are collected at predetermined time points using heparinized Eppendorf tubes. Immediately after collection, the blood samples are placed on ice until centrifuged at 3000 g for 10 min within 1 h. The plasma is collected and stored at −20°C until analysis.

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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 0.9265 mL 4.6327 mL 9.2654 mL 23.1634 mL
    5 mM 0.1853 mL 0.9265 mL 1.8531 mL 4.6327 mL
    10 mM 0.0927 mL 0.4633 mL 0.9265 mL 2.3163 mL
    15 mM 0.0618 mL 0.3088 mL 0.6177 mL 1.5442 mL
    20 mM 0.0463 mL 0.2316 mL 0.4633 mL 1.1582 mL
    DMSO 25 mM 0.0371 mL 0.1853 mL 0.3706 mL 0.9265 mL
    30 mM 0.0309 mL 0.1544 mL 0.3088 mL 0.7721 mL
    40 mM 0.0232 mL 0.1158 mL 0.2316 mL 0.5791 mL
    50 mM 0.0185 mL 0.0927 mL 0.1853 mL 0.4633 mL
    60 mM 0.0154 mL 0.0772 mL 0.1544 mL 0.3861 mL
    80 mM 0.0116 mL 0.0579 mL 0.1158 mL 0.2895 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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    Octreotide acetate Related Classifications

    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:

    Octreotide79517-01-4SMS 201-995Somatostatin ReceptorSSTRsSSTRInhibitorinhibitorinhibit

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