Triptorelin Nasal Spray
2 mg of [D-Trp6]-GnRH as a sterile solution in bacteriostatic water, in a metered spray bottle. Filled from a peptide lot tested in the manufacturer’s own laboratory, with a certificate.
| Compound | Triptorelin [D-Trp6]-GnRH |
|---|---|
| CAS number | 57773-63-4 |
| Molecular formula | C64H82N18O13 |
| Theoretical mass | 1311.5 Da |
| Sequence / structure | pGlu-HWSY-[D-Trp]-LRPG-NH₂ (10 residues; N-terminal pyroglutamate; C-terminal amide) |
| Contents | Triptorelin: 2 mg per bottle (≤ 0.02% w/v) |
| Form | Sterile aqueous solution in bacteriostatic water (0.9% benzyl alcohol), supplied in a metered nasal spray bottle |
| Storage, sealed | Store at 2–8 °C, protected from light; do not freeze |
| Format | Solution in a metered nasal spray bottle |
Sizes and lots
- 2 mg · 1 bottle — $48.99
- 2 mg · Kit of 10 — $435.52
Triptorelin is a GnRH agonist: the ten-residue hypothalamic hormone with D-tryptophan replacing the glycine at position 6. This listing holds 2 mg of triptorelin as a sterile solution in bacteriostatic water, in a metered nasal spray bottle. The research on triptorelin concerns why the position 6 change raises potency, and how GnRH peptides and their tryptophan residues behave in solution; none of the papers cited here studied it through the nose.
What is in the bottle
Each bottle contains 2 mg of triptorelin in a sterile solution of bacteriostatic water with 0.9% benzyl alcohol, at no more than 0.02% w/v according to the safety data sheet. The peptide is the same [D-Trp6]-GnRH, 1311.5 Da, sold in the vial and the pen. The sheet classifies triptorelin as a reproductive toxicant in category 1B (H360); benzyl alcohol is harmful if swallowed or inhaled, irritates the eyes and can sensitize skin.
Store the bottle upright and capped at 2 to 8 °C, away from light, and do not freeze it. The same peptide is sold dry as the triptorelin 2 mg vial, and general guidance on peptide solutions is in peptide storage and stability.
What the research covers
Triptorelin keeps nine of native GnRH's ten residues. Coy and colleagues showed in 1976 that D-amino acids at position 6 raise gonadotropin-releasing activity, the more so with more lipophilic and possibly larger, aromatic side chains, and that [D-Trp6]-LH-RH was 13 times as active as the natural hormone at releasing LH in immature male rats1.
Two findings bear on a product kept in solution. Hahn and colleagues stored synthetic GnRH in solution and found no appreciable loss of activity after four weeks at 4 °C or at room temperature, by both immunoassay and bioassay2. Triptorelin, unlike GnRH, has a second tryptophan, and tryptophan oxidizes: in a hydrogen peroxide model, the pyrrole part of its ring was the most susceptible, and short tryptophan peptides degraded faster than an intact protein3. Neither study used bacteriostatic water or measured triptorelin itself in this format.
None of the papers cited here studied triptorelin given through the nose, so how much of a 1311.5 Da peptide crosses the nasal lining is not established by them. The broader question of peptide sprays is discussed in do peptide nasal sprays work, and the full literature on the compound is in the triptorelin guide.
Frequently asked questions
Is the spray the same peptide as the vial and pen?
Yes, the same [D-Trp6]-GnRH with a theoretical mass of 1311.5 Da. The vial is dry powder stored at −20 °C; the spray and the pen are ready-made solutions in bacteriostatic water, kept at 2 to 8 °C and never frozen.
Has triptorelin been studied as a nasal spray?
Not in the papers cited here. They cover position 6 chemistry and the behaviour of GnRH and tryptophan in solution, and none measured how much triptorelin crosses the nasal lining. There are no findings specific to this format to report.
References
- Coy DH, Vilchez-Martinez JA, Coy EJ, et al. Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6. J Med Chem. 1976;19(3):423-5. DOI · PubMed
- Hahn PM, Van Vugt DA, Reid RL. The stability of synthetic gonadotropin-releasing hormone in solution. Fertil Steril. 1987;48(1):155-8. DOI · PubMed
- Simat TJ, Steinhart H. Oxidation of Free Tryptophan and Tryptophan Residues in Peptides and Proteins. J Agric Food Chem. 1998;46(2):490-498. DOI · PubMed
For laboratory research use only. Not for human or veterinary consumption. Products have not been evaluated by the U.S. Food and Drug Administration and are not intended to diagnose, treat, cure or prevent any disease.