Description

Product Description 

Degarelix acetate hydrate (CAS No. 934246-14-7) is a synthetic decapeptide that functions as a potent, selective, and reversible gonadotropin-releasing hormone receptor (GnRH-R or LHRHR) antagonist. Unlike traditional GnRH agonists, which initially stimulate luteinizing hormone (LH) release before causing receptor desensitization, Degarelix achieves immediate suppression of LH and follicle-stimulating hormone (FSH) without the initial hormone surge. This makes it particularly valuable for research on androgen-dependent tumor growth, prostate cancer models, and reproductive endocrinology.

The compound was originally developed under the identifier FE 200486, and its acetate hydrate salt form provides enhanced solubility and stability for laboratory handling. It binds directly to pituitary GnRH receptors, preventing GnRH signaling and downstream stimulation of gonadotropins. As a result, testicular testosterone synthesis is rapidly suppressed, creating a chemical castration effect in experimental systems.

Key research areas include:

• Prostate cancer models: Studying tumor progression, androgen signaling, and therapeutic resistance mechanisms.

• Endocrine and metabolic regulation: Understanding hypothalamic–pituitary–gonadal (HPG) axis dynamics.

• Reproductive studies: Exploring fertility regulation, gonadotropin suppression, and hormonal modulation.

• Drug synergy research: Combining GnRH antagonists with novel oncological agents in preclinical models.

Degarelix acetate hydrate is manufactured under GMP-compliant conditions, ensuring reproducibility, high peptide purity (>98%), and suitability for both wholesale and retail laboratory supply chains. The lyophilized peptide form guarantees stability during storage and transport.

?? Disclaimer: Degarelix acetate hydrate is supplied strictly for laboratory research use only. It is not intended for human or veterinary administration.

Product Specifications 

This level of detail ensures reproducibility and compliance with modern laboratory quality standards.

Mechanism of Action & Research Applications 

Mechanism of Action

Degarelix acetate hydrate is a GnRH receptor antagonist. In the normal hypothalamic-pituitary-gonadal (HPG) axis, GnRH secreted from the hypothalamus binds to GnRH receptors on pituitary gonadotroph cells. This stimulates secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).

• LH drives testicular Leydig cells to synthesize testosterone.

• FSH regulates Sertoli cell function and spermatogenesis.

In androgen-sensitive tissues (e.g., prostate), testosterone acts as a growth factor. Overproduction or sustained androgen signaling is strongly linked to prostate cancer progression.

Degarelix blocks GnRH receptors directly, preventing GnRH binding and thereby suppressing LH/FSH secretion. The downstream result is:

• Rapid testosterone suppression (within 1–3 days in models).

• No initial flare effect (common with agonists like leuprolide).

• Reversible inhibition upon removal.

This direct antagonism provides a clean model system for exploring androgen deprivation, tumor resistance, and hormonal feedback loops.

Research Applications

1. Prostate Cancer Research

• Study androgen-dependent tumor growth and regression.

• Explore mechanisms of castration resistance.

• Investigate tumor microenvironment changes under GnRH antagonism.

• Evaluate combination therapy with anti-androgens, immunotherapies, or chemotherapy.

2. Endocrine Regulation Studies

• Analyze HPG axis suppression and recovery dynamics.

• Explore effects on gonadotropin release in mammalian models.

• Assess pituitary receptor regulation and downstream hormonal effects.

3. Reproductive Biology

• Study spermatogenesis suppression and fertility regulation.

• Explore GnRH antagonist roles in contraceptive research models.

• Assess reversible endocrine suppression in non-human primates or rodents.

4. Metabolic & Cardiovascular Studies

• Explore testosterone’s role in lipid metabolism and cardiovascular risk.

• Assess endocrine modulation of metabolic pathways.

• Study bone health under long-term androgen suppression.

5. Translational Research

• Model human androgen deprivation therapy (ADT).

• Provide preclinical data for novel oncological therapeutic strategies.

• Explore differences between GnRH agonists vs antagonists.

Potential Side Effects 

In laboratory and preclinical models, Degarelix acetate hydrate demonstrates effects consistent with hormonal suppression. While these are not clinical safety data, researchers should be aware of observed biological responses:

• Endocrine Effects: Reduced testosterone, LH, and FSH; reversible upon withdrawal.

• Reproductive Effects: Suppression of spermatogenesis and fertility in models.

• Metabolic Changes: Altered lipid metabolism, weight changes, and insulin sensitivity shifts.

• Skeletal Effects: Possible reduction in bone mineral density with prolonged use.

• Tumor Dynamics: Rapid tumor regression in androgen-sensitive models, followed by adaptive resistance in some cases.

• Other Observations: Injection-site reactions in vivo studies, mild hepatic enzyme elevation, and altered erythropoiesis.

?? These effects are strictly reported from research models and are intended as references for experimental design. Degarelix acetate hydrate is not a therapeutic agent and must not be used in humans or animals outside laboratory conditions.

Disclaimer

Degarelix acetate hydrate is provided exclusively for laboratory research use only. It is not intended for human or veterinary consumption, administration, or therapeutic purposes. All handling should follow institutional laboratory safety guidelines.

Keywords

• Degarelix acetate hydrate

• Degarelix CAS 934246-14-7

• FE 200486 acetate hydrate peptide

• GnRH receptor antagonist research chemical

• Prostate cancer research peptide

• Endocrine research compound

• GMP supplier Degarelix acetate hydrate

• Laboratory hormonal regulation peptide

• Preclinical androgen deprivation therapy model

• Reproductive endocrinology research tool