What is Ipamorelin?
Ipamorelin (NNC 26-0161) is a synthetic pentapeptide and the first growth hormone secretagogue demonstrated to be fully selective for GH release. Developed by Novo Nordisk and characterized by Raun et al. (1998), ipamorelin activates the growth hormone secretagogue receptor (GHS-R1a) on pituitary somatotrophs without significantly stimulating ACTH, cortisol, prolactin, or aldosterone secretion — a selectivity profile not achieved by earlier GHRPs including GHRP-2, GHRP-6, or hexarelin. The peptide contains an alpha-aminoisobutyric acid (Aib) residue at position 1 and D-2-naphthylalanine at position 3, which contribute to its receptor selectivity and metabolic stability. Ipamorelin does not produce the appetite stimulation associated with GHRP-6 or the ACTH/cortisol co-release seen with other GHRPs, making it the preferred GHSR agonist for research requiring clean GH-specific signaling.
Mechanism of Action
Ipamorelin has been investigated for its selective agonism of GHS-R1a at the pituitary level. Researchers observed that ipamorelin binds and activates GHSR on somatotrophs, triggering Gq-coupled phospholipase C signaling, IP3-mediated calcium release, and GH exocytosis. The critical difference from other GHRPs is that ipamorelin achieves maximal GH release at doses that do not significantly activate GHSR on corticotroph cells (which would release ACTH/cortisol) or lactotroph cells (which would release prolactin). Studies suggest this selectivity may be related to ipamorelin’s binding kinetics and partial agonist activity at GHSR — it may preferentially activate GH-releasing conformational states of the receptor. In dose-response studies, researchers observed a clear separation between the GH-releasing dose-response curve and the cortisol/prolactin curves, providing a wide therapeutic window for selective GH release.
Published Research
Discovery and Selectivity
Raun et al. (1998) characterized ipamorelin as the first GH secretagogue with genuine specificity for GH release. The study demonstrated dose-dependent GH responses without significant ACTH, cortisol, or prolactin elevation across a wide dose range in multiple species [1].
Comparison with Other GHRPs
Hansen et al. (1999) compared ipamorelin with GHRP-6 and GHRP-2 in a head-to-head study. Researchers confirmed ipamorelin’s superior selectivity for GH release with minimal stimulation of non-GH pituitary hormones [2].
Bone Biology
Svensson et al. (2000) investigated ipamorelin in ovariectomized rat models and observed that chronic treatment was associated with changes in bone mineral content and density, establishing ipamorelin’s research utility beyond GH secretion studies [3].
Product Specifications
| Product | Ipamorelin Lyophilized Powder |
|---|---|
| Available Sizes | 10mg, 5mg |
| Purity | ≥99% (HPLC verified) |
| CAS Number | 170851-70-4 |
| Sequence | Aib-His-D-2-Nal-D-Phe-Lys-NH₂ |
| Molecular Formula | C₃₈H₄₉N₉O₅ |
| Molecular Weight | 711.85 g/mol |
| Appearance | White lyophilized powder in glass vial |
| Storage | Store lyophilized at -20°C. Reconstituted solution at 2-8°C, use within 21 days. |
| Testing | Third-party tested — Certificate of Analysis available |
Frequently Asked Questions
Ipamorelin is a synthetic pentapeptide and the first GH secretagogue shown to selectively release GH without significantly affecting cortisol, prolactin, or appetite.
The CAS registry number for Ipamorelin is 170851-70-4.
Unlike GHRP-2, GHRP-6, and hexarelin, ipamorelin releases GH at doses that do not significantly stimulate ACTH, cortisol, prolactin, or appetite pathways.
Store lyophilized Ipamorelin at -20°C. Once reconstituted, store at 2-8°C and use within 21 days.
GHSR agonists (ipamorelin) and GHRH analogs (CJC-1295) act through synergistic pituitary signaling pathways, producing GH release 2-5x greater than either peptide alone.
Ipamorelin produces minimal appetite stimulation compared to GHRP-6 or GHRP-2, which is part of its selectivity advantage.
References
- Raun K, et al. Ipamorelin, the first selective growth hormone secretagogue. Eur J Endocrinol. 1998;139(5):552-561. PMID: 9849822
- Hansen BS, et al. The GH secretagogue ipamorelin: characterization in vitro and in vivo. Growth Horm IGF Res. 1999;9(5):372-373.
- Svensson J, et al. The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats. J Endocrinol. 2000;165(3):569-577. PMID: 10828842
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