Federelin | CAS 57521-78-5 | GnRH Analog for Reproductive and Endocrine Research

Description

Product Description

Federelin, also known as Gonadorelin[6-D-Phe], is a synthetic analog of the endogenous gonadotropin-releasing hormone (GnRH). It has a structural modification at position 6, where the natural amino acid is replaced by D-phenylalanine, enhancing its metabolic stability and receptor affinity. This modification prolongs biological half-life while maintaining potent stimulation of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion from the anterior pituitary.

As a research-grade GnRH agonist, Federelin is widely used in studies of hypothalamic-pituitary-gonadal (HPG) axis regulation, neuroendocrine signaling, and reproductive physiology. Its activity mirrors that of natural GnRH but with improved pharmacodynamic properties, making it ideal for exploring gonadotropin release mechanisms, receptor desensitization, and pituitary feedback loops.

Federelin binds specifically to GnRH receptors (GnRHRs) on pituitary gonadotrophs, initiating G protein–mediated intracellular cascades involving phospholipase C (PLC), inositol triphosphate (IP3), and diacylglycerol (DAG). These cascades elevate intracellular calcium and activate protein kinase C (PKC), leading to exocytosis of LH and FSH.

In experimental settings, Federelin provides a controlled model for understanding reproductive hormone regulation, gonadotropin synthesis, and feedback modulation by sex steroids such as estrogen and testosterone. It also serves as a benchmark in comparative studies evaluating other GnRH analogs, including agonists and antagonists used for hormonal modulation research.

Because of its predictable pharmacology, Federelin is utilized in cellular assays, animal endocrine models, and receptor-binding studies to investigate molecular mechanisms underlying fertility, puberty onset, and reproductive disorders.

Product Specifications

Mechanism of Action

Federelin functions as a GnRH receptor agonist, mimicking the natural pulsatile activity of endogenous gonadotropin-releasing hormone. By binding to pituitary GnRH receptors, Federelin triggers the activation of Gq/11-type G proteins, which stimulate phospholipase C to generate IP3 and DAG. IP3 mobilizes intracellular calcium stores, while DAG activates PKC, culminating in the synthesis and release of LH and FSH from gonadotrophs.

This cascade plays a central role in the hypothalamic-pituitary-gonadal axis, which regulates reproductive function, gametogenesis, and steroidogenesis. In vitro, Federelin demonstrates strong binding affinity to GnRH receptors and sustained receptor activation compared to native GnRH, due to its D-amino acid substitution that resists enzymatic degradation by endopeptidases.

Federelin’s mechanism has also been instrumental in exploring desensitization and downregulation phenomena, where continuous GnRH receptor stimulation reduces gonadotropin output — a concept critical to understanding hormonal suppression therapies. As such, Federelin serves as a model compound for dissecting agonist-induced receptor modulation in endocrine pathways.

Side Effects

While Federelin is well-tolerated in controlled research conditions, continuous or supraphysiological exposure may cause receptor desensitization, transient hormonal fluctuations, or temporary suppression of gonadotropin secretion in experimental organisms.

Potential laboratory-observed effects include:

• Short-term alterations in LH/FSH release

• Cellular feedback inhibition upon sustained exposure

• Minimal off-target receptor interaction

No evidence of cytotoxicity or mutagenicity has been reported. Appropriate handling with standard peptide research protocols is recommended.

Disclaimer

All products are intended for laboratory research use only. Not for human or veterinary use. Researchers must follow institutional biosafety and chemical handling guidelines.

Keywords

Federelin, Gonadorelin[6-D-Phe], GnRH analog, gonadotropin-releasing hormone peptide, endocrine research compound, reproductive biology peptide, LH/FSH modulator, pituitary signaling peptide, neuroendocrine peptide, HPG axis modulator

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