Octreotide Acetate

SKU: orb1303141

Description

Octreotide Acetate is a synthetic, long-acting octapeptide analog of somatostatin. It potently suppresses growth hormone secretion and is widely used in research, including in vitro receptor binding studies and in vivo models of acromegaly and neuroendocrine tumors.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 79517-01-4
• MW: 1079.3
• Purity: 99.62%
• Formula: C₅₁H₇₀N₁₀O₁₂S₂
• SMILES: CC(O)=O.C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1
• Target: Somatostatin
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (4.63 mM);DMSO:255 mg/mL (236.26 mM)

Bioactivity

• In Vivo:
  Groups treated with Octreotide demonstrated a substantial reduction in tumor volume compared to those administered saline. The Octreotide-PPSG formulation (1.4 mg/kg, i.p.) exhibited a superior antitumor effect over the Octreotide-solution (100 μg/kg, i.p.). Furthermore, Octreotide treatments significantly suppressed the expression levels of SSTR2 and SSTR5 in rats with primary HCC, in comparison to the saline group, with Octreotide-PPSG achieving a more pronounced suppression than Octreotide-solution. In addition, a dose of octreotide acetate markedly lowered serum gastrin levels to about a third of the initial levels within 2 hours, maintaining this effect for around 6 hours. On the 21st day, a sustained-release form of octreotide acetate (5 mg intramuscular, every 4 weeks) was introduced.
• Animal Research:
  Octreotide (acetate) is formulated in saline.MiceThirty 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. RatTwelve 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.

Storage & Handling

• Storage: keep away from moisture,store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, Longastatin, Octreotide, Octreotide Acetate, Somatostatin Receptor, SMS 201995, SMS 201-995, SMS 201-995 (acetate), SMS201995, SMS-201995, Sandostatin, SSTR, SSTRs

Compound Identifiers

PubChem CID

6917964