Sermorelin 10mg

Compound Name: Sermorelin

Synonyms: GHRH(1-29), Sermorelin acetate

CAS Number: 86168-78-7

Molecular Formula: C₁₄₉H₂₄₆N₄₄O₄₂S

Molecular Weight: ~3357.96 Da

Structure: Synthetic 29-amino acid peptide

Peptide Sequence: H-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-NH₂

Chemical Structure:

Source: PubChem

Mechanism of Action: Sermorelin acts as a selective agonist of the growth hormone-releasing hormone receptor (GHRH-R), stimulating the pituitary to secrete endogenous growth hormone in a physiologic, pulsatile manner and activating the GH–IGF-1 axis.

Biological Activity: Sermorelin’s agonism at the GHRH receptor effectively stimulates the release of endogenous GH in a pulsatile, physiologic pattern. This leads to increases in circulating IGF-1, with documented benefits in body composition, muscle mass, energy metabolism, and lipid balance. Sermorelin does not suppress natural GH axis regulation and may have better safety for long-term use than recombinant GH.

Storage: −20°C or below. Protect from light and moisture. Avoid repeated freeze-thaw cycles

Drug Categories: Peptides; Growth Hormone Secretagogues; Endocrine Modulators

Additional Notes:

• Typically administered via subcutaneous injection.
• Well-tolerated; may cause transient injection site redness or tingling.
• Does not cross-react with GH receptor or mimic insulin-like actions directly.
• Maintains feedback-sensitive endocrine signaling (GH–IGF-1 axis)

Summary Table:

Disclaimer: For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.

Detailed Product Description

Sermorelin is a synthetic peptide that mimics the first 29 amino acids of endogenous growth hormone-releasing hormone (GHRH), which are sufficient for full biological activity at the pituitary level. As a GHRH receptor agonist, Sermorelin stimulates the hypothalamic-pituitary-somatotropic axis, inducing pulsatile secretion of growth hormone (GH) from the anterior pituitary. This, in turn, activates hepatic production of insulin-like growth factor 1 (IGF-1), mediating anabolic and metabolic effects on muscle, bone, and fat metabolism. Unlike direct recombinant GH therapy, Sermorelin supports physiological feedback loops, maintains the natural rhythm of GH secretion, and reduces the risk of GH receptor downregulation. It is often explored as a more physiologic alternative for treating adult growth hormone insufficiency and age-related declines in GH and IGF-1 levels. Sermorelin has also been shown to increase lean body mass, enhance fat utilization, improve sleep quality, and potentially support gonadotropin release, with emerging use in functional hormone restoration protocols^1-5.

Research Highlights

• Increased Growth Hormone and IGF-1: Studies in adults with age-related GH deficiency show significant increases in pulsatile GH secretion and IGF-1 levels, supporting anabolic and metabolic functions^2,3.
• Improved Body Composition: Sermorelin administration is associated with increases in lean body mass and reductions in body fat, particularly visceral adiposity, in GH-deficient individuals^2,4.
• Preserved Feedback Control: Unlike recombinant GH, sermorelin maintains normal hypothalamic-pituitary feedback, reducing the risk of overtreatment and supporting physiologic hormone rhythms^1,2,4.
• Potential Reproductive Benefits: Preliminary findings suggest sermorelin may modestly enhance LH and testosterone levels, indicating possible utility in male functional hypogonadism⁴.

Mechanism of Action

Sermorelin functions as a synthetic peptide agonist of the growth hormone-releasing hormone receptor (GHRH-R), stimulating the natural secretion of endogenous growth hormone (GH) from the anterior pituitary. By activating this receptor, sermorelin mimics the physiologic effects of endogenous GHRH and initiates the entire growth hormone–insulin-like growth factor 1 (GH–IGF-1) axis^2,4,5.

1. GHRH Receptor (GHRH-R) Agonism

• Stimulates pulsatile growth hormone (GH) secretion: Sermorelin binds to GHRH receptors on pituitary somatotrophs, enhancing cyclic AMP (cAMP) production and activating PKA and MAPK pathways, which trigger physiologic, feedback-sensitive GH release^1-3.
• Elevates circulating IGF-1 levels: GH stimulates hepatic production of IGF-1, which exerts anabolic effects on muscle, bone, and metabolism^1,2,4,5.
• Enhances pituitary responsiveness: Repeated sermorelin administration increases the amplitude and duration of GH pulses, improving long-term axis sensitivity^1,4.
• Supports gonadotropic function: Preclinical and clinical data indicate modest increases in LH and testosterone following sermorelin treatment, possibly due to its upstream modulation of hypothalamic activity^2,3,4.
• Receptor Binding Affinity: High-affinity GHRH receptor agonist; specific EC₅₀ values not widely reported in human systems^1,5.

Pharmacokinetic Profile:

• Route of Administration: Subcutaneous injection
• Dosing Frequency: Once daily
• Half-Life: ~11–12 minutes (plasma); biological activity sustained via pituitary stimulation
• Formulation: Lyophilized acetate salt for reconstitution

Formulation & Handling

• Reconstitute lyophilized powder in sterile bacteriostatic water for injection (0.9% benzyl alcohol)
• Store reconstituted solution at 2–8°C and use within 14 days
• Unreconstituted vials should be stored at −20°C in a dry, light-protected environment
• Avoid repeated freeze-thaw cycles; aliquot as needed for stability
• Stable for up to 12 months when stored properly in lyophilized form

Selected Clinical Trial Activity

Currently, no clinical trials are registered for Sermorelin. Earlier research primarily consisted of investigator-led studies and small-scale trials in adult and pediatric growth hormone insufficiency. While these studies demonstrated favorable outcomes in IGF-1 elevation, body composition, and GH pulsatility, most formal clinical development was discontinued in favor of newer secretagogues. Sermorelin is now predominantly used in off-label and research settings, supported by peer-reviewed literature but not under ongoing regulatory trial evaluation.

References

¹Walker, R.F. et al. Sermorelin: a review of its therapeutic potential in growth hormone insufficiency. Am. J. Ther. 3, 451–462 (1996). https://doi.org/10.2165/00063030-199912020-00007

²Clark, R.V. et al. Effects of GH and GHRH analogs on body composition and hormonal profiles in aging. Aging Male 6, 159–171 (2003). https://doi.org/10.1080/13685530310001616308

³Ishida, Y. & Yamada, S. Growth hormone secretagogues: history, mechanism of action, and clinical development. JCSM Rapid Comm. 3, 206–222 (2020). https://doi.org/10.1002/rco2.31

⁴Walker, R.F. et al. Sermorelin therapy: a physiological approach to adult-onset growth hormone insufficiency. Ther. Adv. Endocrinol. Metab. 9, 149–159 (2018). https://doi.org/10.21037/atm.2019.09.80

⁵Yuen, K.C.J. et al. Pharmacokinetics of growth hormone-releasing hormone analogs in humans. Endocrine 14, 297–302 (2001). https://doi.org/10.1385/ENDO:14:3:297