Octreotide
Based on 16 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 83150-76-9
- Formula: C49H66N10O10S2
- Molecular Weight:1019.24
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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.
Publications Citing Use of MedChemExpress (MCE) Octreotide
More- Mol Cancer. 2024 Sep 20;23(1):205. [Abstract]
- Nat Commun. 2023 Feb 21;14(1):962. [Abstract]
- Eur J Nucl Med Mol Imaging. 2024 Nov;51(13):4099-4110. [Abstract]
- J Ethnopharmacol. 2026 Jun 12:364:121522. [Abstract]
- Biomacromolecules. 2024 May 13;25(5):2749-2761. [Abstract]
- Int J Pharm. 2026 Mar 12:126768. [Abstract]
- Cell Mol Bioeng. 2022 Dec 22;16(1):55-67. [Abstract]
- J Biol Chem. 2025 Jul 30;301(9):110544. [Abstract]
- J Pharm Sci. 2022 Dec;111(12):3417-3423. [Abstract]
- Mol Med Rep. 2024 Jun;29(6):90. [Abstract]
- Basic Clin Pharmacol Toxicol. 2022 Sep;131(3):174-188. [Abstract]
- J Pharm Biomed Anal. 2023 Feb 5:224:115156. [Abstract]
- J Pharm Biomed Anal. 2022 Mar 20:211:114518. [Abstract]
- Patent. US20240307504A1.
- Research Square Print. 2022 Aug.
- University of Helsinki Finland. 2018 Dec.
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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ELISA
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
Biological Activity
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SSTR2 |
SSTR3 |
SSTR5 |
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.
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Cell Line:Human hepatoblastoma HepG2 cell line
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Concentration:10‑8mM
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Incubation Time:6 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 83150-76-9
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Appearance Solid
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Molecular Weight 1019.24
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Formula C49H66N10O10S2
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Color White to off-white
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Synonyms
SMS 201-995
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Sequence
{d-Phe}-Cys-Phe-{d-Trp}-Lys-Thr-Cys-{Threoninol} (Disulfide bridge: Cys2-Cys7)
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Sequence Shortening
{d-Phe}-CF{d-Trp}-KTC-{Threoninol} (Disulfide bridge: Cys2-Cys7)
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Shipping
Room temperature in continental US; may vary elsewhere.
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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.
Publications (16)
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Journal Impact Factor
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Most Recent
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Mol Cancer
FTO-mediated DSP m6A demethylation promotes an aggressive subtype of growth hormone-secreting pituitary neuroendocrine tumors. [Abstract]2024 Sep 20;23(1):205. PMID: 39304899
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.
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Nat Commun
Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine. [Abstract]2023 Feb 21;14(1):962. PMID: 36810324
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.
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Eur J Nucl Med Mol Imaging
Combining [177Lu]Lu-DOTA-TOC PRRT with PARP inhibitors to enhance treatment efficacy in small cell lung cancer. [Abstract]2024 Nov;51(13):4099-4110. PMID: 39023784 -
J Ethnopharmacol
Revealing the temporal metabolic trajectory and potential pharmacodynamic substances of Da-Cheng-Qi Decoction in treating patients with acute pancreatitis: A serum metabolomics-based study. [Abstract]2026 Jun 12:364:121522. PMID: 41825726 -
Biomacromolecules
Investigation of Basolateral Targeting Micelles for Drug Delivery Applications in Polycystic Kidney Disease. [Abstract]2024 May 13;25(5):2749-2761. PMID: 38652072 -
Int J Pharm
Comprehensive design and characterization of pH-gradient-loaded donkey-milk exosomes for oral octreotide delivery: A bench-to-in silico roadmap. [Abstract]2026 Mar 12:126768. PMID: 41831704 -
Cell Mol Bioeng
Combining Metformin and Drug-Loaded Kidney-Targeting Micelles for Polycystic Kidney Disease. [Abstract]2022 Dec 22;16(1):55-67. PMID: 36660586 -
J Biol Chem
2025 Jul 30;301(9):110544. PMID: 40749831 -
J Pharm Sci
Elucidating a Potential Mechanism of Permeability Enhancer Sodium N-[8-(2-hydroxybenzoyl) amino] caprylate in Rats: Evidence of Lymphatic Absorption of Cyanocobalamin Using the Mesenteric Lymph Duct Cannulated Rat. [Abstract]2022 Dec;111(12):3417-3423. PMID: 36228756 -
Mol Med Rep
Octreotide attenuates intestinal barrier damage by maintaining basal autophagy in Caco2 cells. [Abstract]2024 Jun;29(6):90. PMID: 38577927 -
Basic Clin Pharmacol Toxicol
Somatostatin receptor ligands suppressed proliferation and lipogenesis in 3T3-L1 preadipocytes. [Abstract]2022 Sep;131(3):174-188. PMID: 35688794
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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J Pharm Biomed Anal
Analyzing proteolytic stability and metabolic hotspots of therapeutic peptides in two rodent pulmonary fluids. [Abstract]2023 Feb 5:224:115156. PMID: 36463768 -
J Pharm Biomed Anal
Automated high-throughput in vitro assays to identify metabolic hotspots and protease stability of structurally diverse, pharmacologically active peptides for inhalation. [Abstract]2022 Mar 20:211:114518. PMID: 35124452 -
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Solvent & Solubility
H2O : ≥ 50 mg/mL (49.06 mM)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (98.11 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (287 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang XX, et al. Effects of octreotide on hepatic glycogenesis in rats with high fat diet?induced obesity. Mol Med Rep. 2017 Jul;16(1):109-118 [Content Brief]
[2]. Kugita M, et al. Beneficial effect of combined treatment with octreotide and pasireotide in PCK rats, an orthologous model of human autosomal recessive polycystic kidney disease. PLoS One. 2017 May 18;12(5):e0177934. [Content Brief]
[3]. Xiao-Xia Wang,et al. Effects of octreotide on hepatic glycogenesis in rats with high fat diet‑induced obesity. Mol Med Rep. 2017 Jul;16(1):109-118. [Content Brief]
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 |
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| 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.