NAF
Nafarelin Acetate
Cat. No.
BT16879
Source
Synonyms
Appearance
Sterile Filtered White lyophilized (freeze-dried) powder.
Purity
Greater than 98.0% as determined by:
(a) Analysis by RP-HPLC.
(b) Analysis by SDS-PAGE.
(a) Analysis by RP-HPLC.
(b) Analysis by SDS-PAGE.
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
Nafarelin is a decapeptide containing 9 amino acids Glu-His-Trp-Ser-Ala-Leu-Arg-Pro.
Nafarelin is purified by proprietary chromatographic techniques.
Nafarelin is purified by proprietary chromatographic techniques.
Product Specs
Introduction
Nafarelin acetate is a synthetic version of gonadotropin-releasing hormone (GnRH), a hormone naturally found in the body. It works by stimulating the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from the pituitary gland, leading to a temporary increase in the production of ovarian hormones.
Description
Nafarelin is a peptide made up of 9 amino acids: Glu-His-Trp-Ser-Ala-Leu-Arg-Pro. It is purified using specialized chromatographic methods.
Physical Appearance
White, freeze-dried powder that has been sterilized by filtration.
Formulation
The protein is freeze-dried at a concentration of 1 mg/ml without any additional ingredients.
Solubility
To prepare for use, it is recommended to first dissolve the freeze-dried Nafarelin in sterile, high-purity water (18 MΩ-cm) at a concentration of at least 100 µg/ml. This solution can then be diluted further with other aqueous solutions as needed.
Stability
Although the freeze-dried Nafarelin remains stable for up to 3 weeks at room temperature, it should be stored in a dry environment below -18°C. After reconstitution, the solution should be stored at 4°C for no more than 2-7 days. For long-term storage, it is recommended to freeze it below -18°C. Adding a carrier protein (0.1% HSA or BSA) is recommended for long-term storage. Avoid repeated freezing and thawing.
Purity
The purity of Nafarelin is greater than 98%, as determined by two methods: (a) analysis using reversed-phase high-performance liquid chromatography (RP-HPLC) and (b) analysis using sodium dodecyl-sulfate polyacrylamide gel electrophoresis (SDS-PAGE).
Product Science Overview
Chemical Structure and Properties
Mechanism of Action
Nafarelin acetate functions by initially stimulating the release of the pituitary gonadotropins, luteinizing hormone (LH), and follicle-stimulating hormone (FSH). This stimulation results in a temporary increase in gonadal steroidogenesis. However, with repeated dosing, the stimulatory effect on the pituitary gland is abolished, leading to decreased secretion of gonadal steroids. This reduction in steroid levels causes tissues and functions dependent on these hormones to become quiescent .
Clinical Uses
- Endometriosis: Nafarelin acetate is used to manage endometriosis by reducing estrogen levels, which helps in alleviating the symptoms associated with this condition .
- Central Precocious Puberty: It is effective in treating central precocious puberty by delaying the onset of puberty in children .
- Uterine Fibroids: The medication helps in shrinking uterine fibroids by lowering estrogen levels .
- IVF: Nafarelin acetate is used to control ovarian stimulation during in vitro fertilization procedures .
- Transgender Hormone Therapy: It is also used as part of hormone therapy for transgender individuals .
Administration and Dosage
Side Effects
Pharmacokinetics
- Bioavailability: When administered intranasally, nafarelin acetate has a bioavailability of approximately 2.8% .
- Protein Binding: It has a protein binding rate of 80% .
- Metabolism: The compound is metabolized by peptidases and not by the cytochrome P450 enzymes .
- Elimination Half-life: The elimination half-life of nafarelin acetate is about 2.5 to 3.0 hours when administered intranasally .
- Excretion: It is excreted through urine (44-55%) and feces (19-44%) .
Nafarelin acetate represents a significant advancement in the treatment of hormone-related conditions, offering a targeted approach to managing symptoms and improving patient outcomes.
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