OCT Human

Octreotide Human
Cat. No.
BT16965
Source
Synonyms
Appearance
Sterile Filtered White lyophilized (freeze-dried) powder.
Purity
Greater than 98.0% as determined by RP-HPLC.
Usage
Prospec's products are furnished for LABORATORY RESEARCH USE ONLY. The product may not be used as drugs, agricultural or pesticidal products, food additives or household chemicals.
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Description

Octreotide Human Synthetic is a single, non-glycosylated, polypeptide chain containing 8 amino acids, having a molecular mass of 1019.26 Dalton and a molecular formula of C49H66N10O10S2.
Octreotide is purified by proprietary chromatographic techniques.

Product Specs

Introduction
Octreotide acetate is a synthetic analog of somatostatin, a naturally occurring hormone. It is longer acting than somatostatin and works by inhibiting the release of certain hormones, including growth hormone and gastro-entero-pancreatic peptide hormones.
Description
Octreotide Human Synthetic is a single-chain polypeptide that is not glycosylated. It consists of 8 amino acids and has a molecular weight of 1019.26 Daltons. Its molecular formula is C49H66N10O10S2. Octreotide is purified using proprietary chromatographic techniques.
Physical Appearance
White powder that has been freeze-dried and sterilized by filtration.
Formulation
The Octreotide was freeze-dried from a solution with a concentration of 1mg/ml. No additives were used in the formulation.
Solubility
To reconstitute the freeze-dried Octreotide, it is recommended to dissolve it in sterile 18MΩ-cm H2O at a concentration of at least 100 µg/ml. This solution can then be further diluted in other aqueous solutions.
Stability
Lyophilized Octreotide is stable at room temperature for up to 3 weeks, but it is recommended to store it in a dry environment below -18°C. Once reconstituted, Octreotide should be stored at 4°C for 2-7 days. For long-term storage, it is recommended to freeze it below -18°C. To preserve its stability during long-term storage, consider adding a carrier protein like 0.1% HSA or BSA. Avoid repeated freeze-thaw cycles.
Purity
The purity of this product is greater than 98.0% as determined by RP-HPLC.
Amino Acid Sequence
H-D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-L-threoninol.

Product Science Overview

Chemical Structure and Properties

Octreotide has a complex chemical structure with the formula C49H66N10O10S2 and a molar mass of 1019.25 g/mol . It is available in several forms, including subcutaneous, intramuscular, intravenous, and oral formulations .

Mechanism of Action

Octreotide works by binding to somatostatin receptors, predominantly SSTR2 and SSTR5 . This binding inhibits the release of several hormones and decreases exocrine secretions in the gastrointestinal tract . It also reduces splanchnic blood flow and chyle flow .

Medical Uses

Octreotide is used to treat a variety of conditions, including:

  • Acromegaly: A disorder caused by excess growth hormone, leading to abnormal growth of body tissues .
  • Carcinoid Syndrome: A condition associated with carcinoid tumors that secrete vasoactive substances, causing flushing and diarrhea .
  • VIPomas: Tumors that secrete vasoactive intestinal peptide, leading to severe diarrhea .

In addition to these, octreotide is also used to manage symptoms related to other hormone-secreting tumors .

Approval and Availability

Octreotide was approved for medical use in the United States in 1988 . It is available under various brand names, including Sandostatin, Bynfezia Pen, and Mycapssa . Notably, Mycapssa is the first and only oral somatostatin analog approved by the FDA for long-term maintenance treatment of acromegaly .

Pharmacokinetics

The bioavailability of octreotide varies depending on the route of administration, with 60% bioavailability when administered intramuscularly and 100% when administered subcutaneously . It has a protein binding rate of 40-65% and is metabolized primarily in the liver . The elimination half-life of octreotide ranges from 1.7 to 1.9 hours, and it is excreted mainly through urine (32%) .

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