Gonadorelin

Product Overview

Gonadorelin is a synthetic decapeptide identical in amino acid sequence to endogenous mammalian gonadotropin-releasing hormone (GnRH), also known as luteinizing hormone-releasing hormone (LHRH) . With the primary structure pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH₂, this peptide serves as the master regulator of the reproductive endocrine axis .

Unlike longer-acting synthetic GnRH analogs (e.g., leuprolide, goserelin), gonadorelin retains the native decapeptide sequence without amino acid substitutions. It exhibits an ultrashort plasma half-life of approximately 4 minutes, making it uniquely suited for research requiring precise pulsatile stimulation of the hypothalamic-pituitary-gonadal (HPG) axis .

Gonadorelin is recognized in pharmacopoeias under names including Factrel®, Cystorelin®, and Kryptocur® . It is FDA-approved as a prescription drug for human use under specific diagnostic and therapeutic indications.

⚠️ Research Context: While gonadorelin is an approved pharmaceutical, this product is offered for research purposes only. It is not intended for human consumption, diagnostic use, therapeutic application, or clinical administration. It is intended solely for qualified researchers and scientific institutions.

Mechanism of Action

Gonadorelin binds specifically to GnRH receptors (GnRHR) on anterior pituitary gonadotroph cells, activating a G-protein coupled receptor (GPCR)-mediated signaling cascade .

Primary Signaling Pathway (Gαq/11 – PLC)

1. G-protein Activation: Gonadorelin activates the Gαq/11 family of G-proteins .

2. Phospholipase C (PLC) Stimulation: This activates PLC, which hydrolyzes phosphatidylinositol 4,5-bisphosphate (PIP₂) into two second messengers: inositol 1,4,5-trisphosphate (IP₃) and diacylglycerol (DAG) .

3. Calcium Release: IP₃ triggers the release of stored intracellular calcium (Ca²⁺) from the endoplasmic reticulum .

4. PKC Activation: DAG, along with elevated Ca²⁺, activates Protein Kinase C (PKC) .

5. MAPK Cascades: Downstream, gonadorelin stimulates Mitogen-Activated Protein Kinase (MAPK) pathways, including ERK, JNK, and p38, which regulate gonadotropin subunit gene transcription .

6. Gonadotropin Release: This cascade stimulates the synthesis and pulsatile release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) .

Critical Pharmacodynamic Distinction

Secondary Signaling: cGMP Pathway

Gonadorelin is known to stimulate cAMP production in some in vitro models (EC₅₀ ≈ 1 nM), suggesting crosstalk between the PLC and cAMP pathways that warrants further investigation .

Key Research Applications:

• Pulsatile GnRH receptor signaling studies

• Hypothalamic-pituitary-gonadal (HPG) axis research

• Reproductive endocrinology and gonadotropin regulation

• Receptor binding and second messenger investigations

• Comparative studies with modified GnRH analogs

Product Specifications

Quality Control Specifications

Certificate of Analysis (COA) available upon request.

Research Background

Structural Characteristics

Gonadorelin is a decapeptide with the following key features :

• C-terminal modification: Proline-amide at position 10

• N-terminal modification: Pyroglutamate (pGlu) at position 1

• Key residues for receptor binding: His², Trp³, Tyr⁵, Arg⁸

Native GnRH vs. Superagonist Analogs

Gonadorelin is structurally and pharmacokinetically distinct from synthetic superagonists such as leuprolide, buserelin, goserelin, and triptorelin :

Preclinical Research Findings

In Vitro Receptor Activation:

• Receptor Binding Affinity (Kd): GnRH binds to rat pituitary cells with Kd ≈ 50 nM .

• Inositol Phosphate Production: EC₅₀ ≈ 11 nM in rat anterior pituitary cells .

• LH Release (EC₅₀): Gonadorelin acetate stimulates LH release in pituitary cell cultures with EC₅₀ of 0.1–1 nM .

• MAPK Activation (LβT2 cells): GnRH (100 nM) activates ERK (~60-fold at 10 min), p38 (~30-fold at 10 min), and JNK (~10-fold at 30 min) .

Endocrine Effects in Fish Research (Tambaqui, 2025):
A study published in 2025 on tambaqui (an Amazonian fish) showed that:

• Gonadorelin (60 μg/kg) suppressed fshβ transcription in females (p=0.021) .

• No effect on lhβ transcription in either sex .

• Elevated plasma levels of E2, 17α-OHP, and testosterone .

• 67% of treated females ovulated; none of the controls did .

• The downregulation of fshβ may promote final oocyte maturation by favoring a hormonal environment with increased progesterone influence . gonadorelin dosing

Pharmacokinetic Properties

Clinical and Regulatory Context

• FDA Status: Approved as a prescription drug for diagnostic evaluation of pituitary function and for ovulation induction in hypothalamic amenorrhea .

• Veterinary Use: Approved for treatment of ovarian cysts and fertility improvement in cattle; estrus synchronization .

• Regulatory Classification: US. Gonadorelin is available as gonadorelin hydrochloride (Factrel®) and gonadorelin diacetate tetrahydrate (Cystorelin®) for injectable use .

Storage & Reconstitution Guidelines

Storage Conditions:

• Lyophilized (Long-term): -20°C, protected from light, dry, sealed

• Lyophilized (Short-term): 2°C – 8°C (refrigerated)

• Reconstituted: 4°C for up to 7 days; aliquot and store at -20°C for extended storage; avoid repeated freeze-thaw cycles

Reconstitution Protocol:

1. Allow vial to reach room temperature

2. Add sterile 18 MΩ-cm H₂O or bacteriostatic water

3. Gently swirl (do not vortex) until fully dissolved

4. Dispense into individual aliquots to minimize freeze-thaw degradation

Note: Peptides are sensitive to formulation, process, and environmental conditions that may lead to aggregation and degradation.

Important Notice

⚠️ FOR RESEARCH USE ONLY

This product is not intended for human consumption, diagnostic use, therapeutic application, or clinical administration. Gonadorelin is a research chemical intended exclusively for in-vitro and laboratory research purposes.

• Not a dietary supplement, food additive, or pharmaceutical for over-the-counter purchase

• Although clinically approved, this product is sold for research-grade applications only

• Intended solely for qualified researchers and scientific institutions

By purchasing this product, you confirm that you are a licensed researcher or laboratory professional and agree to use this compound in compliance with all applicable local, national, and international regulations.

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Gonadorelin Peptide 2mg – ≥98% Purity
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