Deslorelin

Deslorelin
Cat. No.
BT15979
Source
Synonyms
Appearance
Sterile Filtered White lyophilized (freeze-dried) powder.
Purity

Greater than 99.0% as determined by RP-HPLC.

Usage
THE BioTek'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

Deslorelin is a potent LHRH/GnRH agonist has a molecular formula of C64H83N17O12, pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-NHC2H5  having an Mw of 1284.4 Dalton.

Product Specs

Introduction
Deslorelin, a gonadotropin-releasing hormone analog, is under investigation for cancer treatment due to its potential to suppress sex hormone production in the ovaries or testicles. In equine medicine, it is utilized for ovulation induction in mares. Deslorelin exerts its effects by binding to and activating gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland. Continuous and prolonged administration of deslorelin leads to desensitization of pituitary GnRH receptors, thereby inhibiting the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This ultimately results in a substantial decrease in testosterone production in males and estradiol production in females.
Description
Deslorelin, a potent LHRH/GnRH agonist, is characterized by a molecular formula of C64H83N17O12, with a peptide sequence of pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-NHC2H5. It has a molecular weight of 1284.4 Daltons.
Physical Appearance
Upon lyophilization, Deslorelin presents as a sterile, white, and finely textured powder.
Formulation
The Deslorelin peptide undergoes lyophilization without the addition of any other substances.
Solubility
To reconstitute lyophilized Deslorelin, it is recommended to dissolve it in sterile 18MΩ-cm H2O at a concentration not less than 100µg/ml. This solution can be further diluted with other aqueous solutions if required.
Stability
Lyophilized Deslorelin demonstrates stability at room temperature for a period of 3 weeks. However, for optimal long-term storage, it is recommended to store the desiccated product at a temperature below -18°C. Upon reconstitution, Deslorelin should be stored at 4°C for a period of 2 to 7 days. For storage beyond 7 days, it is advisable to store it at -18°C. To enhance long-term stability, consider adding a carrier protein, such as 0.1% HSA or BSA. It is important to avoid repeated cycles of freezing and thawing.
Purity
The purity of Deslorelin is determined to be greater than 99.0% using Reverse Phase High-Performance Liquid Chromatography (RP-HPLC).

Product Science Overview

Chemical Structure and Properties

Deslorelin is a peptide with the chemical formula C64H83N17O12 and a molar mass of approximately 1282.47 g/mol . It is a GnRH superagonist, meaning it has a much higher potency compared to natural GnRH .

Mechanism of Action

Deslorelin works by initially stimulating the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland. This initial surge is followed by a downregulation of GnRH receptors, leading to a decrease in LH and FSH levels over time . This mechanism is utilized to control reproductive functions in animals.

Veterinary Uses

Deslorelin is used in various species, including horses, dogs, and ferrets. Some of its primary applications include:

  • Inducing Ovulation: In mares, deslorelin is used to induce ovulation, allowing for optimal timing of artificial insemination .
  • Managing Reproductive Functions: In dogs, it is used to manage reproductive functions and can be used to prevent pregnancy .
  • Treating Adrenal Disease: In ferrets, deslorelin is used to manage adrenal disease .
Commercial Forms

Deslorelin is available under several brand names, including Suprelorin and SucroMate . These products are typically administered as implants or injectable suspensions.

Regulatory Status

In the United States, deslorelin is FDA-approved for use in mares and ferrets. Its use in other species or for other indications is considered off-label and is subject to regulatory restrictions .

Preparation and Administration

Deslorelin is administered either intramuscularly or subcutaneously. The implants release the hormone over a period of time, typically around 72 hours . It is important to follow veterinary guidance for proper administration and dosage.

Side Effects and Precautions

Common side effects include swelling, sensitivity, and redness at the injection site. In rare cases, prolonged estrus and uterine infections have been reported in dogs . Pregnant women or those intending to become pregnant should handle deslorelin with caution to avoid direct contact with the medication .

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