Histrelin
Histrelin
Cat. No.
BT16435
Source
Synonyms
Appearance
Sterile Filtered White lyophilized (freeze-dried) powder.
Purity
Greater than 99.0% as determined by(a) Analysis by RP-HPLC.
(b) Analysis by SDS-PAGE.
(b) Analysis by SDS-PAGE.
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
Histrelin has a molecular formula of C66H86N18O12, a.a. sequence of Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt and having a Mw of 1323.32 Dalton.
Product Specs
Introduction
Histrelin, a hormone functionally similar to one naturally produced by the brain's hypothalamus gland, reduces estrogen and testosterone levels in the bloodstream. It's important to note that estrogen suppression can impact bone health, potentially leading to decreased density or slowed growth. As a potent LHRH agonist, histrelin acetate stimulates LH and FSH release while curbing the effects of sex steroids on male and female reproductive systems. Continuous administration, after an initial increase, leads to a downregulation of LH and FSH levels, subsequently suppressing ovarian and testicular steroid production. Histrelin's effectiveness, both in living organisms and laboratory settings, is comparable to its D-Trp6-containing counterpart. Its high water solubility and enhanced lipophilic nature make it a promising candidate for clinical use.
Description
Histrelin, with a molecular weight of 1323.32 Daltons, is characterized by a molecular formula of C66H86N18O12 and an amino acid sequence of Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt.
Physical Appearance
When freeze-dried, Histrelin presents as a sterile, white powder.
Formulation
The Histrelin peptide undergoes lyophilization without any additional substances.
Solubility
For reconstitution of lyophilized Histrelin, sterile 18MΩ-cm H2O is recommended, with an initial concentration of at least 100 μg/ml. Further dilutions can be prepared using other aqueous solutions.
Stability
While lyophilized Histrelin remains stable at room temperature for up to three weeks, it's best stored in a dry environment below -18°C. After reconstitution, Histrelin should be kept at 4°C for a period of 2-7 days. For extended storage, freezing below -18°C is recommended, ideally with the addition of a carrier protein like 0.1% HSA or BSA. Repeated freezing and thawing should be avoided.
Purity
Histrelin boasts a purity exceeding 99.0%, as verified through two methods: (a) Reverse-Phase High-Performance Liquid Chromatography (RP-HPLC) analysis and (b) Sodium Dodecyl Sulfate-Polyacrylamide Gel Electrophoresis (SDS-PAGE) analysis.
Product Science Overview
Chemical Structure and Properties
Histrelin is a synthetic peptide that mimics the natural gonadotropin-releasing hormone. Its chemical formula is C66H86N18O12, and it has a molar mass of approximately 1323.528 g/mol . The structure of histrelin allows it to bind effectively to GnRH receptors, leading to its potent biological effects.
Mechanism of Action
When histrelin is present in the bloodstream, it acts on specific cells in the pituitary gland known as gonadotropes. It stimulates these cells to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH). Over time, continuous stimulation by histrelin leads to a downregulation of GnRH receptors, resulting in decreased production of LH and FSH. This mechanism makes histrelin an effective GnRH agonist .
Medical Uses
Histrelin is used to treat various hormone-sensitive conditions:
- Prostate Cancer: Histrelin is used in the palliative treatment of advanced prostate cancer. It helps reduce testosterone levels, which can slow the growth of prostate cancer cells .
- Central Precocious Puberty (CPP): Histrelin is effective in treating CPP in children. It helps delay the onset of puberty by reducing the levels of sex hormones .
- Uterine Fibroids: In women, histrelin can be used to manage uterine fibroids by reducing estrogen levels .
- Transgender Youth: Histrelin is sometimes used off-label to suppress puberty in transgender children and adolescents until they are ready to begin cross-sex hormone therapy .
Administration
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