Description

Abarelix Acetate (PPI 149 Acetate; R 3827 Acetate; CAS 547741-72-0) is a synthetic decapeptide GnRH receptor antagonist that competes with endogenous GnRH for receptor binding, thereby suppressing gonadotropin release (LH, FSH) and reducing testosterone synthesis. This mechanism avoids the initial hormone “flare” commonly seen with GnRH agonists—a critical advantage in prostate cancer models where hormone surges can exacerbate disease .

Manufactured under GMP standards with a verified purity of 99.89%, Abarelix Acetate ensures reproducibility and high-quality results in preclinical and mechanistic studies. Its receptor-binding affinity (Kd ~ 0.8 nM) and capacity for rapid testosterone suppression make it ideal for studies exploring androgen deprivation, hormone-dependent tumor suppression, and endocrine signaling pathways.

Though discontinued clinically in the U.S., Abarelix remains an invaluable tool in research, particularly for modeling symptomatic advanced prostate cancer and novel GnRH antagonist effects without flare. Wholesale and retail quantities are available with comprehensive quality documentation. For laboratory research use only. Not for human or veterinary applications.

Product Specifications

Mechanism of Action & Research Applications

Abarelix Acetate functions as a competitive antagonist at GnRH receptors, inhibiting GnRH-stimulated secretion of LH and FSH. This leads to a rapid and sustained drop in testosterone levels—critical for investigating androgen-dependent cellular processes. Unlike agonists, Abarelix avoids the initial surge in testosterone (“flare”) that can worsen prostate cancer symptoms—a key advantage for experimental modeling .

Research Applications:

• Prostate Cancer Models – Evaluating effects of androgen deprivation without initial hormone flare.

• Hormonal Regulation Studies – Peptide control of LH/FSH secretion.

• Endocrine Feedback Mechanisms – Exploring downstream pituitary and gonadal responses.

• Comparative GnRH Antagonist Studies – Benchmarking Abarelix versus current agents (e.g., degarelix, relugolix).

• Animal Model Development – Investigating castration-resistant pathways and hormone-independent growth.

Development & Research Background

Abarelix was one of the first GnRH antagonists developed to bypass limitations of agonist therapy. Early clinical use provided rapid testosterone suppression without a surge, but infrequent allergic reactions led to its limited approval and eventual withdrawal in certain markets .

However, its pharmacodynamic profile—rapid onset, potent suppression, peptide-based mechanistic clarity—makes it a gold standard research comparator. It helped define the benefits of receptor antagonism, catalyzed the development of newer agents, and remains important for investigating GnRH pathway modulation in endocrine and cancer research models.

Side Effects

(Note: Listed for experimental reference only.)

In preclinical and clinical data:

• Possible allergic reactions—reported in rare patients after injection (not applicable to research use) .

• Hypogonadism signature effects—decrease in testosterone-related physiology in animal models.

• Liver enzyme elevations and prolonged QT interval observed—dose-dependent and model-specific—should be monitored in long-term in vivo studies .

Disclaimer

Abarelix Acetate is provided for laboratory research use only, not for human or veterinary use. It must be handled and disposed of according to institutional safety protocols. Researchers are responsible for ensuring compliance with applicable laws and guidelines.

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