Sermorelin acetate
[CAS# 114466-38-5]

Identification

• Classification: API >> Other chemicals
• Name: Sermorelin acetate
• Synonyms: (3S)-4-[[(1S)-2-[[(1S,2S)-1-[[(1S)-2-[[(1S,2R)-1-[[(1S)-3-amino-1-[[(1S)-2-[[(1S)-2-[[(1S)-1-[[(1S)-5-amino-1-[[(1S)-1-[[(1S)-1-[[2-[[(1S)-4-amino-1-[[(1S)-1-[[(1S)-2-[[(1S)-2-[[(1S)-1-[[(1S)-5-amino-1-[[(1S)-1-[[(1S)-1-[[(1S)-4-amino-1-[[(1S)-2-[[(1S,2S)-1-[[(1S)-1-[[(1S)-2-[[(1S)-1-carbamoyl-4-guanidino-butyl]amino]-1-(hydroxymethyl)-2-oxo-ethyl]carbamoyl]-3-methylsulfanyl-propyl]carbamoyl]-2-methyl-butyl]amino]-1-(carboxymethyl)-2-oxo-ethyl]carbamoyl]-4-oxo-butyl]carbamoyl]-3-methyl-butyl]carbamoyl]-3-methyl-butyl]carbamoyl]pentyl]carbamoyl]-4-guanidino-butyl]amino]-1-methyl-2-oxo-ethyl]amino]-1-(hydroxymethyl)-2-oxo-ethyl]carbamoyl]-3-methyl-butyl]carbamoyl]-4-oxo-butyl]amino]-2-oxo-ethyl]carbamoyl]-3-methyl-butyl]carbamoyl]-2-methyl-propyl]carbamoyl]pentyl]carbamoyl]-4-guanidino-butyl]amino]-1-[(4-hydroxyphenyl)methyl]-2-oxo-ethyl]amino]-1-(hydroxymethyl)-2-oxo-ethyl]carbamoyl]-3-oxo-propyl]carbamoyl]-2-hydroxy-propyl]amino]-1-benzyl-2-oxo-ethyl]carbamoyl]-2-methyl-butyl]amino]-1-methyl-2-oxo-ethyl]amino]-3-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-4-oxo-butanoic acid
• Molecular Formula: C₁₄₉H₂₄₆N₄₄O₄₂S^.C₂H₄O₂
• Molecular Weight: 3417.97
• CAS Registry Number: 114466-38-5
• SMILES: [H]/N=C(\N)NCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCSC)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN/C(N)=N/[H])NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN/C(N)=N/[H])NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)CC)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(N)=O

Properties

• Density: 1.5±0.1 g/cm³ Calc.^*
• Index of refraction: 1.65 (Calc.)^*

^* Calculated using Advanced Chemistry Development (ACD/Labs) Software.

Discovory and Applicatios

Sermorelin acetate is a synthetic peptide that was developed as an analog of a naturally occurring human hypothalamic hormone involved in the regulation of growth hormone secretion. The compound is derived from the first 29 amino acids of human growth hormone releasing hormone, which is the biologically active region responsible for stimulating the pituitary gland to release endogenous growth hormone. The discovery of growth hormone releasing hormone in the late 1970s and early 1980s clarified the hypothalamic control of pituitary growth hormone secretion and provided the foundation for the development of shorter, stable synthetic fragments such as sermorelin. By isolating and characterizing the active portion of the native hormone, researchers were able to design peptides that retained biological activity while being more suitable for pharmacological use.

Sermorelin was synthesized to mimic the physiological action of endogenous growth hormone releasing hormone rather than directly supplying growth hormone itself. This approach was based on the understanding that stimulation of the pituitary could preserve normal regulatory feedback mechanisms. Early experimental and clinical studies demonstrated that sermorelin could induce pulsatile growth hormone release when administered to humans, confirming that the truncated peptide maintained functional interaction with pituitary receptors. These findings supported its use as a diagnostic and therapeutic tool in endocrinology.

The primary application of sermorelin acetate has been in the evaluation and management of disorders related to growth hormone secretion. It has been used clinically as a diagnostic agent to assess pituitary growth hormone reserve, particularly in pediatric patients with suspected growth hormone deficiency. By measuring growth hormone response following administration of sermorelin, clinicians can differentiate between hypothalamic and pituitary causes of impaired growth hormone secretion. This diagnostic role reflects its close resemblance to the natural regulatory hormone and its ability to provoke a controlled physiological response.

In addition to diagnostic use, sermorelin acetate has been applied therapeutically, especially in pediatric endocrinology. It has been administered to children with growth hormone deficiency linked to inadequate hypothalamic stimulation rather than irreversible pituitary failure. In this context, sermorelin promotes endogenous growth hormone release, supporting normal growth patterns while maintaining the body’s intrinsic regulatory systems. Compared with direct growth hormone replacement, this strategy was considered advantageous for preserving feedback control and potentially reducing certain risks associated with exogenous hormone administration.

Beyond pediatric applications, sermorelin has been investigated in adults for its effects on growth hormone dynamics, body composition, and metabolic parameters. Research has examined its influence on age related decline in growth hormone secretion and its potential role in studying growth hormone physiology in adults. These investigations contributed to a broader understanding of growth hormone regulation, even where clinical use remained limited.

Sermorelin acetate also became an important research tool in neuroendocrinology. Its use in experimental settings has helped clarify the mechanisms of growth hormone release, receptor activation, and downstream signaling pathways. Because it selectively targets growth hormone secretion without directly supplying the hormone, it has been valuable for dissecting hypothalamic pituitary interactions and for studying the temporal patterns of hormone release.

Over time, the clinical landscape evolved with the availability of recombinant human growth hormone and other diagnostic agents, leading to a decline in the widespread therapeutic use of sermorelin. Nevertheless, its development represents a significant milestone in peptide hormone research and endocrine pharmacology. Sermorelin acetate illustrates how understanding the structure and function of natural regulatory hormones can lead to targeted synthetic analogs that advance both clinical practice and fundamental biological research.

References

Prakash A, Goa KL (1999) Sermorelin: a review of its use in the diagnosis and treatment of children with idiopathic growth hormone deficiency. BioDrugs 12(2) 139–157 DOI: 10.2165/00063030-199912020-00007

Granata R, Leone S, Zhang X, Sha W, Hare JM, Schally AV, Ghigo E (2025) Growth hormone‑releasing hormone and its analogues in health and disease. Nature Reviews Endocrinology 21 180–195 DOI: 10.1038/s41574-024-01052-1