Ipamorelin 5mg

Compound Name: Ipamorelin

Synonyms: 170851-70-4, NNC-26-0161, UNII-Y9M3S784Z6

CAS Number: 170851-70-4

Molecular Formula: C₃₈H₄₉N₉O₅

Molecular Weight: ~711.86 g/mol

Structure: Synthetic pentapeptide

Peptide Sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH₂

Chemical Structure:

Source: PubChem

Mechanism of Action: Ipamorelin is a selective agonist of the ghrelin receptor (GHS-R1a), stimulating the release of endogenous growth hormone (GH) from the anterior pituitary. It mimics the physiologic effects of natural ghrelin without affecting cortisol, prolactin, or ACTH levels. Through targeted activation of GHS-R1a, ipamorelin initiates the GH–IGF-1 axis while preserving natural hormone pulsatility^1-4.

Biological Activity: Ipamorelin stimulates a dose-dependent increase in circulating GH and subsequent rise in IGF-1. It demonstrates high in vivo potency in both animal and human models with a well-tolerated safety profile^1,4. Ipamorelin shows promise as a motilin agonist in gastrointestinal contexts and has been evaluated for postoperative ileus therapy².

Storage: Store lyophilized powder at –20°C. Reconstituted solutions should be stored at 2–8°C and used within 30 days.

Drug Categories: Growth Hormone Secretagogue (GHS); Ghrelin Receptor Agonist; Synthetic Peptide; Research Peptide

Additional Notes:

Ipamorelin is supplied for research purposes only and is not approved for therapeutic use. It has shown favorable pharmacokinetics, including reduced desensitization and absence of cortisol stimulation seen in earlier GHRPs.

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

Ipamorelin is a synthetic GHS derived from the pentapeptide class of ghrelin mimetics. It acts as a potent and selective agonist at the GHS-R1a receptor. Unlike traditional GHRPs such as hexarelin and GHRP-6, ipamorelin does not stimulate ACTH, prolactin, or cortisol secretion, thereby reducing off-target hormonal side effects¹.It shows strong pharmacodynamic activity, evidenced by marked GH peaks following intravenous administration in both preclinical and human models². Clinical investigations have demonstrated its tolerability and utility in contexts like growth hormone deficiency, frailty, and gastrointestinal dysmotility. Notably, ipamorelin was evaluated in a randomized trial for management of postoperative ileus, where it showed numerically shorter recovery times for gastrointestinal function⁴.

Research Highlights

• Selective ghrelin receptor (GHS-R1a) agonist, minimal ACTH or cortisol release¹
• Stimulates dose-dependent GH and IGF-1 elevation²
• Exhibits high in vivo potency (ED₅₀ ~2.3 nmol/kg)⁴
• Maintains physiologic GH pulsatility with minimal desensitization³

• Investigated for prokinetic effects in postoperative ileus (GI-2 improvement in open-laparotomy patients)²

Mechanism of Action

Ipamorelin acts as a selective ghrelin receptor (GHS-R1a) agonist to stimulate the endogenous release of growth hormone (GH) from pituitary somatotrophs¹.

GHS-R1a Activation

• Selective endocrine activity: Elevates GH and IGF-1 levels without significantly increasing ACTH, cortisol, or prolactin, a limitation observed in earlier GHSs like GHRP-6 and hexarelin³.
• Gastrointestinal prokinetic effects: In clinical studies, ipamorelin accelerated recovery of upper and lower GI tract function post-surgery, likely through motilin-like agonism and central regulation².
• Ipamorelin shows high receptor affinity with an ED₅₀ of ~2.3 nmol/kg in pigs⁴

Pharmacokinetic Profile:

• Route of Administration: Intravenous, subcutaneous (experimental)
• Dosing Frequency: Twice daily
• Half-Life: Short (~2 hours); dependent on route and formulation
• Formulation: Lyophilized powder for reconstitution

Formulation & Handling

• Lyophilized peptide powder, reconstituted in sterile PBS or water.
• Store lyophilized peptide at –20 °C; upon reconstitution, aliquot and freeze at –80 °C to avoid degradation.
• Avoid repeated freeze–thaw cycles.

Selected Clinical Trial Activity

References

¹Hansen TK, et al. Highly potent growth hormone secretagogues: hybrids of NN703 and Ipamorelin. Bioorg Med Chem Lett 11 (14):1915–1918 (2001).

²Jogaro VS et al., Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers. Pharm Res. 16(9): 1412-1416 (1999).

³Raun, K. et al. Ipamorelin, the first selective growth hormone secretagogue. Eur. J. Endocrinol. 139, 552–561 (1998).

⁴Beck, DE, et al. Prospective, randomized, controlled, proof-of-concept study of the ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients. Int. J. Colorectal Dis. 29, 1527–1534 (2014).