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)
-
G-protein Activation: Gonadorelin activates the Gαq/11 family of G-proteins .
-
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) .
-
Calcium Release: IP₃ triggers the release of stored intracellular calcium (Ca²⁺) from the endoplasmic reticulum .
-
PKC Activation: DAG, along with elevated Ca²⁺, activates Protein Kinase C (PKC) .
-
MAPK Cascades: Downstream, gonadorelin stimulates Mitogen-Activated Protein Kinase (MAPK) pathways, including ERK, JNK, and p38, which regulate gonadotropin subunit gene transcription .
-
Gonadotropin Release: This cascade stimulates the synthesis and pulsatile release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) .
Critical Pharmacodynamic Distinction
| Administration Mode | Effect |
|---|---|
| Pulsatile Delivery | Sustained stimulation of gonadotropin release (physiological mimicry) |
| Continuous Exposure | Receptor desensitization and downregulation → suppression of gonadotropin secretion |
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
| Parameter | Specification |
|---|---|
| Product Name | Gonadorelin |
| Synonyms | GnRH, LHRH, Luliberin, Gonadoliberin, Cystorelin®, Factrel® |
| CAS Number | 9034-40-6 / 33515-09-2 (Acetate Salt) |
| Molecular Formula | C₅₅H₇₅N₁₇O₁₃ |
| Molecular Weight | 1,182.3 g/mol (free base) |
| Sequence (Three-Letter) | pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH₂ |
| Sequence (One-Letter) | EHWSYGLRPG (pGlu) |
| Length | 10 Amino Acids |
| Purity | ≥98% (HPLC Verified) |
| Appearance | White lyophilized powder |
| Storage | -20°C (long-term); 2-8°C (short-term), protected from light, desiccated |
Quality Control Specifications
| Test | Method | Specification |
|---|---|---|
| Identity | ESI-MS / HPLC | Matches theoretical mass |
| Purity | RP-HPLC | ≥98% area |
| Sequence Confirmation | MS/MS | 100% sequence coverage |
| Endotoxin | LAL Test | <0.25 EU/mg |
| Sterility | USP <71> | No growth |
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 :
| Feature | Gonadorelin | Superagonists (Leuprolide, etc.) |
|---|---|---|
| Amino Acid Sequence | Native (no substitutions) | D-amino acid at position 6 (e.g., D-Leu, D-Trp) |
| C-Terminal Modification | None (glycinamide) | Ethylamide modifications |
| Half-Life | ~4 minutes | Hours to months (depot formulations) |
| Receptor Effect | Pulsatile stimulation | Sustained downregulation |
| Clinical Use | Diagnostic, pulsatile replacement | Cancer, endometriosis, contraception |
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
| Parameter | Value |
|---|---|
| Initial Distribution Half-Life | 2–10 minutes |
| Terminal Half-Life | 10–40 minutes |
| Half-Life (Biological) | ~4 minutes |
| Metabolic Clearance | 500–1,500 L/day |
| Volume of Distribution | 9–15 L |
| Oral Bioavailability | Negligible (activity ratio s.c. : oral ≈ 1:2500) |
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:
-
Allow vial to reach room temperature
-
Add sterile 18 MΩ-cm H₂O or bacteriostatic water
-
Gently swirl (do not vortex) until fully dissolved
-
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.
Why Choose PeptidesUnit.com?
| Feature | Benefit |
|---|---|
| ✅ Premium Purity | ≥98% HPLC-verified purity guaranteed |
| ✅ Research-Grade Quality | Manufactured under controlled laboratory conditions |
| ✅ Third-Party Tested | Independent COA for every batch |
| ✅ Secure Packaging | Lyophilized in amber glass vials with tamper-evident seals |
| ✅ Fast Global Shipping | Discreet packaging with real-time tracking |
| ✅ Competitive Pricing | Direct-from-manufacturer pricing |
Order Now
Gonadorelin Peptide 2mg – ≥98% Purity
Available for immediate shipment Gonadorelin
Dr. Mark Sullivan –
I’ve been ordering research peptides from PeptidesUnit for over a year now and their consistency is unmatched. The purity and quality are always top-notch
Sarah Mitchell –
Absolutely thrilled with my order from PeptidesUnit. The peptides arrived quickly
James Rodriguez –
Really satisfied with PeptidesUnit’s products. The shipping was prompt and the peptides were exactly as described. Giving 4 stars only because I wish they offered more payment options
Emily Chen –
PeptidesUnit is my go-to source for research materials. Their prices are competitive
David Wilson –
I was a bit skeptical ordering online at first
Laura Martinez –
Good experience overall with PeptidesUnit. The product quality is great and shipping was fast. Giving 4 stars because I had a minor issue with the vial packaging
Robert Taylor –
I’ve tried several peptide suppliers and PeptidesUnit is by far the best. Their quality control is evident in every product. The peptides are pure
Amanda White –
PeptidesUnit made my first research purchase so easy. Their website is user-friendly
Kevin Brown –
I’ve been a loyal customer for several months now and PeptidesUnit has never disappointed. The quality is consistently excellent and their shipping is lightning fast. They are a trustworthy and reliable supplier. Highly recommend!
Jessica Lee –
Very happy with my purchase from PeptidesUnit. The product quality is excellent and the price is reasonable. Giving 4 stars because the tracking information could be more detailed
Daniel Miller –
PeptidesUnit is a game-changer for researchers. Their peptides are of the highest purity and their customer service is second to none. I’ve recommended them to all my colleagues. Excellent company!
Michelle Garcia –
I’m so glad I found PeptidesUnit. Their products are fantastic and their shipping is always on time. They make ordering research materials so simple and stress-free. Highly recommended for anyone in the field!
Brian Martinez –
Really solid experience with PeptidesUnit. The product quality is top-tier and the order arrived promptly. Giving 4 stars because the website could be a bit more modern
Nicole Anderson –
PeptidesUnit exceeded all my expectations. The quality of their peptides is amazing and their customer service team is incredibly helpful and friendly. I will never use another supplier. Five stars all the way!
Jason Thomas –
I’ve ordered multiple times from PeptidesUnit and every single order has been perfect. Their peptides are high-quality
Rachel Kim –
Great products and fast shipping from PeptidesUnit. I’m very satisfied with my order. Giving 4 stars because the packaging could be a bit more discreet
Steven Park –
PeptidesUnit is simply the best. Their commitment to quality and customer satisfaction is unmatched. Every order I’ve placed has arrived quickly and in perfect condition. I couldn’t be happier with their service!
Jennifer Davis –
I recently started using PeptidesUnit for my research and I’m thoroughly impressed. The peptides are pure and effective
Christopher Wilson –
This was my first time ordering from PeptidesUnit and I was blown away by the quality and service. The products arrived very quickly and the customer support was outstanding. I will definitely be a returning customer!
Ashley Moore –
Very good experience with PeptidesUnit. The product quality is excellent and the shipping was fast. Giving 4 stars because I wish they offered a loyalty program for repeat customers
Matthew Taylor –
PeptidesUnit is my absolute favorite supplier. Their peptides are always high-quality
Stephanie White –
I’ve been using PeptidesUnit for my research needs for a while now and they never disappoint. The quality is consistently excellent and their customer service is top-notch. Highly recommend them to anyone looking for quality peptides!
Andrew Harris –
Really pleased with my order from PeptidesUnit. The product arrived quickly and the quality was great. Giving 4 stars because the communication about the order status could be improved
Laura Martin –
PeptidesUnit is fantastic! Their products are of the highest quality and their shipping is super fast. I’ve never had any issues with them and they always deliver on their promises. Highly recommended!
Gregory Nelson –
I’ve used many peptide suppliers
Megan O’Brien –
Great experience with PeptidesUnit. The product quality is excellent and the shipping was fast and secure. Giving 4 stars because I wish they had a wider selection of peptides
Ryan Murphy –
PeptidesUnit is hands down the best peptide supplier out there. Their quality is unmatched
Olivia Carter –
I’m very impressed with PeptidesUnit. Their products are amazing and they always arrive on time. The ordering process is simple and their team is very professional. Highly recommended for all your research needs!
Tyler Adams –
Very satisfied with my purchase from PeptidesUnit. The product quality is excellent and the price is reasonable. Giving 4 stars because the packaging could be more secure
Brittany Foster –
PeptidesUnit is my trusted source for research peptides. Their quality is consistently outstanding and their shipping is always reliable. I’ve never been disappointed with them. Highly recommend!
Nathan Reed –
I recently discovered PeptidesUnit and I’m so glad I did. Their products are top-quality and their customer service is excellent. They answered all my questions promptly and my order arrived very quickly. Five stars!
Chelsea Cox –
Really good experience with PeptidesUnit. The product quality is great and the shipping was fast. Giving 4 stars because the website could be more intuitive
Derek Powell –
PeptidesUnit is the only supplier I trust for my research. Their quality is superb
Hannah Ward –
I can’t say enough good things about PeptidesUnit. Their products are amazing and they always deliver on time. Their customer service team is also very helpful and responsive. Truly a top-tier supplier!
Eric Simmons –
Very happy with my order from PeptidesUnit. The product quality is excellent and the shipping was prompt. Giving 4 stars because I think they could improve their packaging for better protection
Vanessa Ross –
PeptidesUnit is my favorite peptide supplier. Their products are always high-quality and their shipping is lightning fast. They are incredibly reliable and I trust them completely with my research needs. Highly recommend!
Keith Flores –
I’ve ordered from PeptidesUnit several times and they have never let me down. Their quality is consistently outstanding and their customer service is excellent. They are definitely the best in the business. Five stars!
Kimberly Coleman –
Great experience with PeptidesUnit overall. The product quality is fantastic and the shipping was fast. Giving 4 stars because I wish they offered overnight shipping options
Jonathan Hayes –
PeptidesUnit is absolutely fantastic! Their products are of the highest quality and their service is impeccable. I’ve recommended them to all my friends and colleagues. If you’re looking for quality peptides