Description: What is Ipamorelin?
Ipamorelin is a synthetic pentapeptide and a selective growth hormone secretagogue (GHS). It functions as a ghrelin receptor agonist (GHS-R1a) and was developed to stimulate the release of growth hormone (GH) from the pituitary gland [1][6].
Unlike early growth hormone-releasing peptides (GHRPs), ipamorelin is characterized by its high selectivity and lack of significant stimulation of cortisol, prolactin, or acetylcholine. It was designed to mimic the GH-releasing activity of ghrelin without the appetite-stimulating and metabolic side effects typically associated with other secretagogues [1][6].
Chemically, ipamorelin contains a 2-methylalanyl residue at the N-terminus, a D-2-naphthylalanyl residue, and a D-phenylalanyl residue, which contribute to its stability and receptor selectivity [4].
Regulatory & Research Use Notice:
Ipamorelin is classified as a research chemical. According to FDA records, it is not approved for human therapeutic use [4]. Suppliers explicitly state: "For research use only, not for human or veterinary use". Clinicians and researchers should be aware that while preclinical studies suggest a favorable safety profile, rigorous human efficacy data remain limited, and no FDA-approved indications exist [2][6].
Biochemical & Physical Parameters
| Parameter | Specification |
|---|---|
| IUPAC Name | 2-Methylalanyl-L-histidyl-3-(2-naphthyl)-D-alanyl-D-phenylalanyl-L-lysinamide |
| Sequence | Aib-His-D-2-Nal-D-Phe-Lys-NH₂ |
| UNII | Y9M3S784Z6 |
| InChIKey | NEHWBYHLYZGBNO-BVEPWEIPSA-N |
| Physical Form | Solid at 20°C |
| Melting Point | 74-83°C |
| Terminal Half-Life | Approximately 2 hours (human, IV administration) |
| Clearance | 0.078 L/h/kg |
| Volume of Distribution (Vdss) | 0.22 L/kg |
| Peak GH Stimulation | ~0.67 hours post-administration |
| Storage Stability | Powder: 3 years at -20°C; 2 years at 4°C |
Reviews
Mechanism of Action
Ipamorelin acts as a selective agonist at the growth hormone secretagogue receptor (GHS-R1a), also known as the ghrelin receptor. Binding to this receptor triggers a signaling cascade that results in the release of growth hormone (GH) from somatotroph cells in the anterior pituitary [1][6].
Key Pharmacodynamic Characteristics:
- Selective GH Stimulation: Ipamorelin induces a dose-dependent increase in GH levels, with peak concentrations observed approximately 40 minutes after administration. Unlike older GHRPs (e.g., GHRP-2, GHRP-6), ipamorelin does not significantly elevate plasma levels of cortisol, prolactin, adrenocorticotropic hormone (ACTH), or aldosterone [1][6].
- Episodic Release: The GH response to ipamorelin manifests as a single episode of release, with GH levels returning to baseline within a few hours. This mimics the natural pulsatile pattern of GH secretion [3].
- Ghrelin-Mimetic Effects: As a ghrelin receptor agonist, ipamorelin also exhibits prokinetic effects in the gastrointestinal tract. It has been studied for its ability to enhance gastric emptying and postoperative gastrointestinal motility [1][5].
- Indirect Response Model: Pharmacokinetic-pharmacodynamic modeling indicates that ipamorelin induces GH production via a zero-order release rate over a finite duration, with a half-maximal stimulatory concentration (SC₅₀) of 214 nmol/L [3].
Benefits & Functional Advantages (Based on Research Applications)
1. Growth Hormone Stimulation
Selective GH Release: Preclinical and human volunteer studies confirm that ipamorelin reliably stimulates GH secretion without off-target hormonal effects [3][6].
Favorable Half-Life: With a 2-hour terminal half-life, ipamorelin allows for controlled dosing schedules in research protocols [3].
2. Gastrointestinal Motility
Prokinetic Activity: In phase 2 clinical studies, ipamorelin was investigated for postoperative ileus management, demonstrating prokinetic effects in the gastrointestinal tract [1].
Safety Profile: In a randomized controlled trial of 117 patients receiving bowel resection, ipamorelin (0.03 mg/kg twice daily for up to 7 days) was well tolerated, with adverse event rates comparable to placebo (87.5% vs 94.8%) [1].
3. Research Advantages
High Purity (≥98%): Suitable for in vivo and in vitro research applications requiring consistent quality .
Stable Under Recommended Storage: When stored at -20°C, the peptide maintains integrity for extended periods.
No Significant CYP Interactions: The peptide is not known to interact with major cytochrome P450 enzymes, reducing confounding factors in drug interaction studies.
Applications
1. Research & Development
Endocrinology Studies: Investigation of GH secretion pathways, aging-related GH decline, and pituitary function.
Metabolic Research: Evaluation of GH's effects on body composition, fat metabolism, and insulin sensitivity.
Gastrointestinal Motility: Preclinical models of postoperative ileus, gastroparesis, and constipation [1][5].
Muscle Wasting & Cachexia: Studies exploring GH secretagogues for sarcopenia and cancer cachexia [2].
2. Combination Research
CJC-1295 + Ipamorelin: This combination is frequently studied in research settings. CJC-1295 (a GHRH analog) provides sustained GH-releasing activity, while ipamorelin offers pulsatile stimulation. Murine models suggest improved outcomes in glucocorticoid-induced muscle loss, though human data are lacking [2].
3. Sports Medicine & Regenerative Research
A 2026 narrative review in the American Journal of Sports Medicine identified ipamorelin as one of several peptides gaining attention in orthopaedic and sports medicine research. However, the authors emphasize that definitive human clinical data are absent, and significant research is required before clinical recommendations can be made [2].
FAQ: Frequently Asked Questions
Q: Ipamorelin vs. Tesamorelin: What's the difference?
A: Tesamorelin is a GHRH analog approved by the FDA for treating HIV-associated lipodystrophy [2]. Ipamorelin is a ghrelin mimetic with a different mechanism of action and is not FDA-approved. While both stimulate GH release, tesamorelin has a longer half-life and established clinical indication, whereas ipamorelin remains primarily in the research domain [2][6].
Q: Ipamorelin vs. CJC-1295: How do they compare?
A: CJC-1295 is a synthetic analog of GHRH that provides sustained GH release through bioconjugation with a half-life of 6-8 days. Ipamorelin acts via the ghrelin receptor with a 2-hour half-life. In research settings, they are sometimes studied in combination to achieve both basal and pulsatile GH stimulation [2]. However, neither is FDA-approved for therapeutic use.
Q: What is the typical ipamorelin dosage in research?
A: In published clinical studies, intravenous doses of 0.03 mg/kg twice daily were administered [1]. For subcutaneous administration in research protocols, dosages vary widely; researchers should refer to peer-reviewed literature for context-specific guidance. No standardized dosing exists for human use outside of approved clinical trials.
Q: What are the side effects of ipamorelin?
A: In the phase 2 postoperative ileus study (n=114), treatment-emergent adverse events occurred in 87.5% of the ipamorelin group vs 94.8% in the placebo group, indicating that reported events were largely attributable to the surgical setting rather than the study drug [1]. Common theoretical considerations include injection site reactions, transient flushing, and potential increases in appetite (though less than with other GHRPs). Long-term safety data are not available.
Q: Is ipamorelin legal? Can I buy it in Singapore or elsewhere?
A: Regulatory status varies by jurisdiction. In the United States, ipamorelin is not FDA-approved and is legally available only for research purposes (not for human consumption). Suppliers typically restrict sales to qualified research institutions and do not ship to residential addresses. Singapore has strict regulations on peptides; researchers should consult local health authorities before procurement.
Q: What is ipamorelin peptide used for?
A: In research settings, ipamorelin is used to study GH secretion, gastrointestinal motility, and metabolic pathways. It is not approved for clinical use, despite widespread promotion in the direct-to-consumer "peptide therapy" market [2][6].
Q: Is ipamorelin bad for you?
A: The safety profile of ipamorelin in controlled short-term studies appears acceptable [1]. However, long-term safety data in humans are lacking. The 2025 review in The Journal of Sexual Medicine concluded that "clinical efficacy and safety profile remains underreported with need for rigorous, high-quality RCTs and long-term studies" [6].
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Usage Disclaimer
This product is intended exclusively for research purposes in controlled laboratory environments. It is not intended for diagnostic, therapeutic, or human use. Purchasers must ensure compliance with all applicable regulations governing research materials. Xi'an Huilin Biological Technology Co., Ltd. assumes no liability for misuse or unauthorized handling of this material.
References
- Beck, D.E., Sweeney, W.B., & McCarter, M.D. (2014). Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients. International Journal of Colorectal Disease, 29(12), 1527-1534.
- Mayfield, C.K., et al. (2026). Injectable Peptide Therapy: A Primer for Orthopaedic and Sports Medicine Physicians. The American Journal of Sports Medicine, 54(1), 223-229.
- Gobburu, J.V.S., Agersø, H., Jusko, W.J., & Ynddal, L. (1999). Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers. Pharmaceutical Research, 16(9), 1412-1416.
- U.S. Food and Drug Administration. (2026). *IPAMORELIN - UNII: Y9M3S784Z6*. FDA Substance Registration System.
- Venkova, K., Mann, W., Nelson, R., & Greenwood-Van, M.B. (2009). Efficacy of ipamorelin, a novel ghrelin mimetic, in a rodent model of postoperative ileus. Journal of Pharmacology and Experimental Therapeutics, 329(3), 1110-1116.
- Arora, R., Venkatesh, A., Krishingner, G.A., & Campbell, K. (2025). Peptides in Practice: Evaluating Efficacy and Safety in Men's Health. The Journal of Sexual Medicine, 22(Supplement 4), qdaf320.196.
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