Gonadorelin Technical Specification Sheet

Molecular Properties

Parameter Value
Chemical Name Gonadotropin-Releasing Hormone / Luteinizing Hormone-Releasing Hormone (LHRH)
Amino Acid Sequence pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH₂
Molecular Formula C₅₅H₇₅N₁₇O₁₃
Molecular Weight 1182.31 g/mol
CAS Number 33515-09-2
Sequence Length 10 amino acids (decapeptide)
Receptor Target GnRH receptor (GnRHR) on pituitary gonadotrophs

Physical Properties

Property Specification
Appearance White to off-white lyophilized powder
Solubility Soluble in water, PBS (pH 7.0-7.4), or 0.9% saline at ≥1 mg/mL
pH (1% solution) 5.0 - 7.0
Hygroscopicity Low; standard desiccated storage acceptable
Solution Stability Stable at 4°C for 7-10 days; degradation at room temperature within 24-48h

Analytical Specifications

Test Specification
HPLC Purity ≥98.0%
Mass Spectrometry Confirmed [M+H]⁺ = 1182.31 ± 0.5 Da
Peptide Content ≥95% (by amino acid analysis)
Endotoxin Level <1.0 EU/mg
Acetate Content ≤5%
TFA Content ≤0.1%
Water Content ≤6% (Karl Fischer)

Storage Parameters

Condition Specification
Lyophilized Storage -20°C, desiccated
Lyophilized Shelf Life 24-36 months when stored properly
Reconstituted Storage 2-8°C for up to 10 days; -20°C for up to 3 months
Reconstitution Protocol Add 1.0 mL sterile water or PBS to 1 mg vial; vortex gently for 30 seconds
Freeze-Thaw Cycles Maximum 3 cycles; aliquot for single use recommended
Light Sensitivity Minimal; standard laboratory storage acceptable

Research Dosing Reference

Application Typical Dose Range Frequency Route
In Vitro Pituitary Cell Assays 1-100 nM Acute stimulation (minutes to hours) Culture media
Small Animal Models (Rodent) 10-100 μg/kg (10-100 nmol/kg) Single dose or pulsatile (every 60-90 min) IV, SC, IP
LH/FSH Stimulation Test 25-100 μg/kg Single bolus IV or SC
Reproductive Axis Studies 0.1-10 μg/animal Pulsatile every 1-2 hours IV infusion pump or bolus
Note: Dosing information is for research reference only. Gonadorelin is intended strictly for in vitro and animal research. Pulsatile administration mimics physiological secretion pattern.

Key Research Studies

Year Study Focus Key Findings
1971 Discovery and characterization First isolation and sequencing of GnRH from porcine and ovine hypothalami; demonstrated decapeptide structure with pGlu N-terminus and Gly-NH₂ C-terminus critical for activity
1982 Pulsatile secretion pattern and receptor dynamics Established that pulsatile GnRH delivery (60-90 min intervals) maintains gonadotropin secretion while continuous administration causes receptor desensitization and downregulation within 7-14 days
1997 Structure-activity relationship Systematic amino acid substitutions revealed positions 1, 2, 3, 6, and 10 essential for receptor binding; modifications at positions 6 and 10 generated superagonists with 50-200x potency
2008 GnRH receptor signaling cascades Detailed GnRHR signaling via Gq/11 → PKC activation → Ca²⁺ mobilization → ERK1/2 phosphorylation pathway; demonstrated EC₅₀ of 0.5-2 nM for LH secretion from primary pituitary cells

Mechanism of Action

Biological Pathway Description
Receptor Binding Binds GnRH receptor (GnRHR), a Gq-coupled GPCR on anterior pituitary gonadotrophs; high affinity with Kd ~1-5 nM
Signal Transduction Activates phospholipase C → IP₃/DAG production → intracellular Ca²⁺ release → protein kinase C activation
Gonadotropin Secretion Stimulates rapid release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from gonadotrophs within 5-15 minutes
Pulsatile Requirement Physiological pulses every 60-120 minutes maintain LH/FSH; continuous exposure desensitizes receptors and suppresses gonadotropin output
Half-Life 2-4 minutes (IV); rapid degradation by hypothalamic and pituitary peptidases

Clinical Variants and Analogs

Type Examples Key Modification
Native GnRH Gonadorelin acetate Natural sequence; short half-life
Superagonists Triptorelin, Leuprolide, Goserelin Position 6 and 10 substitutions; extended half-life and potency
Antagonists Cetrorelix, Ganirelix, Degarelix Multiple D-amino acid substitutions; competitive receptor blockade
Diagnostic Forms Gonadorelin hydrochloride Alternative salt form for injection; equivalent activity

Quality Control Parameters

Test Method Acceptance Criteria
Appearance (visual) White to off-white powder; no aggregation or discoloration
Reconstitution Test Complete dissolution within 1 minute; clear colorless solution
RP-HPLC (purity) Main peak ≥98.0%; no single impurity >0.5%
ESI-MS (identity) Observed [M+H]⁺ within ±0.05% of theoretical 1182.31 Da
Peptide Sequence Confirmation N-terminal pGlu and C-terminal Gly-NH₂ verified by MS/MS

External References

1. Schally AV, et al. Isolation and properties of the FSH and LH-releasing hormone. Biochem Biophys Res Commun. 1971;43(2):393-9. https://pubmed.ncbi.nlm.nih.gov/4930860/

2. Conn PM, Crowley WF Jr. Gonadotropin-releasing hormone and its analogs. Annu Rev Med. 1994;45:391-405. https://www.annualreviews.org/doi/10.1146/annurev.med.45.1.391

3. National Center for Biotechnology Information. PubChem Compound Summary for Gonadorelin. https://pubchem.ncbi.nlm.nih.gov/compound/Gonadorelin

Disclaimer: This product is intended for research use only. Not for human or veterinary diagnostic or therapeutic use. Handle according to institutional biosafety protocols.