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Type
Synthetic peptide (linear decapeptide, 10 residues)
Molecular formula
C55H75N17O13
Molecular weight
~1,182.3 Da
CAS number
33515-09-2
Amino acids
10
Sequence
pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH₂
Modification
Pyroglutamate (pGlu) at the N-terminus; C-terminal glycinamide amidation. Both modifications are critical for receptor recognition and confer relative resistance to aminopeptidase and carboxypeptidase cleavage; primary plasma degradation occurs at the Gly6 position.
Gonadorelin is a synthetic linear decapeptide that engages a seven-transmembrane Gq/G11-coupled class A GPCR as a structural binding partner. The cognate receptor is unusual among GPCRs in lacking a cytoplasmic C-terminal tail, a structural feature that slows β-arrestin-mediated internalization and is studied as the basis for frequency-dependent receptor behavior. Upon ligand binding, the structurally characterized coupling proceeds through phospholipase C-β, which hydrolyzes PIP₂ into IP₃ and DAG; IP₃ mobilizes intracellular Ca²⁺ and DAG activates protein kinase C in cell-based assay models. A defining property characterized in the literature is pulse-dependent receptor pharmacology: intermittent exposure and continuous receptor occupancy produce distinct receptor states, with sustained occupancy driving GRK-mediated phosphorylation, β-arrestin recruitment, receptor internalization, and progressive surface-density downregulation. The pyroglutamate N-terminus and C-terminal glycinamide are essential for receptor recognition and confer relative resistance to exopeptidase cleavage; primary plasma degradation occurs at the Gly6 position, contributing to ultrashort circulatory clearance.
Lyophilized
20°C (−80°C recommended for long-term)
lyophilized powder stable approximately 24 months under proper conditions.
Hygroscopic; keep sealed and dry. Protect from light and moisture. Aliquot to minimize freeze-thaw exposure.
Reviews
Naelitz BD, Momtazi-Mar N, Lundy SD, et al. (2025). Nature Reviews Urology
Robin G, Dumont A, et al. (2014). Gynécologie Obstétrique & Fertilité
Reviews
Flanagan CA, Manilall A (2017). Front Endocrinol (Lausanne)
Naor Z, Harris D, Shacham S (1998). Front Neuroendocrinol
Naor Z (2009). Front Neuroendocrinol
Stamatiades GA, Carroll RS, Kaiser UB (2019). Endocrinology
McArdle CA, Franklin J, Green L, Hislop JN (2002). J Endocrinol
McArdle CA, Davidson JS, Willars GB (1999). Mol Cell Endocrinol
Constantin S, Bjelobaba I, Stojilkovic SS (2022). Curr Opin Pharmacol
Plant TM (2019). F1000Res
Okamura H, Tsukamura H, Ohkura S, et al. (2013). Adv Exp Med Biol
Boehm U, Bouloux PM, Dattani MT, et al. (2015). Nat Rev Endocrinol
Fanis P, Neocleous V, Papapetrou I, Phylactou LA, Skordis N (2023). Int J Mol Sci
Clinical
Sun QH, Zheng Y, Zhang XL, Mu YM (2015). Chin Med J (Engl)
Kim YJ, Hwangbo J, Park KH, et al. (2024). Ann Pediatr Endocrinol Metab
Quaas P, Quaas AM, Fischer M, De Geyter C (2022). J Assist Reprod Genet
Hao M, Mao JF, Guan QB, et al. (2021). Ann Transl Med
Primary research
Mao JF, et al. (2017). Asian Journal of Andrology
Willars GB, Heding A, Vrecl M, et al. (1999). J Biol Chem
Hislop JN, Everest HM, Flynn A, et al. (2001). J Biol Chem
Pawson AJ, Faccenda E, Maudsley S, et al. (2008). Endocrinology
Caunt CJ, Hislop JN, Kelly E, et al. (2004). Endocrinology
Burger LL, Dalkin AC, Aylor KW, Haisenleder DJ, Marshall JC (2002). Endocrinology
Lim S, Pnueli L, Tan JH, Naor Z, Rajagopal G, Melamed P (2009). PLoS One
Also known as: GnRH, GnRH-I, LHRH, gonadoliberin, luliberin
View this compound in the Research Library →Frequently Bought Together