Ipamorelin

Also known as: NNC 26-0161

Ipamorelin is a selective growth hormone secretagogue and ghrelin receptor agonist. Research documents its highly selective GH-releasing properties with minimal effect on cortisol, prolactin, or ACTH in preclinical models.

Ipamorelin
For Research Use Only

Structure

Aib-His-D-2Nal-D-Phe-Lys-NH2 (pentapeptide)

Molecular Weight

711.9 Da

Target Receptor

GHSR-1a (ghrelin receptor)

Selectivity

Minimal ACTH, cortisol, prolactin stimulation

Developer

Novo Nordisk (NNC 26-0161)

Research Use Only

Not for human or veterinary use

Overview

Ipamorelin is a synthetic pentapeptide developed as a growth hormone secretagogue (GHS) and selective agonist of the ghrelin receptor (GHSR-1a). It was synthesized in the late 1990s by Novo Nordisk (compound NNC 26-0161) as part of a research program to develop GHS compounds with improved selectivity profiles. Unlike earlier secretagogues such as GHRP-6 or GHRP-2, ipamorelin demonstrates highly specific stimulation of GH release with minimal cross-activation of other pituitary axes.

The selectivity of ipamorelin is its defining research characteristic. In preclinical studies using rat pituitary cell cultures and in vivo models, ipamorelin produced robust dose-dependent GH release while showing negligible effects on plasma ACTH, cortisol, or prolactin — hormones that are frequently co-stimulated by less selective GHS compounds. This selectivity makes ipamorelin a valuable pharmacological tool for research designs that require isolated modulation of the GH/IGF-1 axis.

Research with ipamorelin has been conducted across several model systems. Studies in aged animal models have documented the ability of ipamorelin to partially restore GH pulse amplitude that declines with aging. Additional research has examined its effects on bone mineral density in animal models, with findings of increased bone formation markers. Ipamorelin has also been used as a reference compound in receptor pharmacology studies characterizing GHSR-1a binding.

Ipamorelin is available for in vitro and in vivo preclinical research use only and is not approved for human therapeutic application. Researchers designing GH axis studies will find ipamorelin's selectivity profile particularly useful for isolating GH-specific effects from confounding changes in stress-axis hormones.

Mechanism of Action

Ipamorelin binds and activates the growth hormone secretagogue receptor 1a (GHSR-1a), a G-protein coupled receptor expressed on somatotroph cells of the anterior pituitary. Receptor activation triggers Gq/11-mediated phospholipase C activation, leading to IP3-mediated calcium release and PKC activation, which collectively stimulate GH granule exocytosis.

Unlike ghrelin, which also activates GHSR-1a, ipamorelin's synthetic pentapeptide structure confers high selectivity for pituitary somatotrophs over other GHSR-expressing tissues, explaining its minimal orexigenic and HPA-activating effects at standard research doses. The compound does not appear to stimulate somatostatin release, distinguishing it mechanistically from GHRH-based secretagogues.

Research Applications

Research Use Only. Ipamorelin is available for laboratory and research applications only. It is not approved by the FDA or any equivalent regulatory authority for human or veterinary therapeutic use. All information on this page is derived from published preclinical literature and is presented for informational and research context purposes only. Investigators should consult current primary literature and comply with applicable regulations before initiating research.

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Peptide Family

Growth Hormone Secretagogues

GHRH Receptor · GH/IGF-1 Axis · GH Secretagogue Research

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