Ipamorelin – Selective Growth Hormone Secretagogue for Endocrine Research
Basic Information
Product Name: Ipamorelin (INN)
CAS Number: 170851-70-4
Synonyms: NNC 26-0161, NNC-26-0161
Molecular Formula: C₃₈H₄₉N₉O₅
Molecular Weight: ~711.85–711.9 g/mol
Appearance: White lyophilized powder
Purity: ≥98% (HPLC)
Sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH₂ (pentapeptide)
Storage: Powder at –20°C for up to 3 years
Packaging: Available in vials (1 mg, 2 mg, 5 mg, 10 mg)
Overview
Ipamorelin is a synthetic pentapeptide and a potent, selective agonist of the ghrelin/growth hormone secretagogue receptor (GHS-R1a). Originally developed by Novo Nordisk (investigated for postoperative ileus, later discontinued due to lack of efficacy), it has since become a widely used tool in endocrine and metabolic research due to its ability to stimulate growth hormone (GH) release from the pituitary gland.
Mechanism of Action
Ipamorelin mimics ghrelin and binds to the ghrelin receptor (GHS-R1a) in the brain, primarily through activation of ghrelin receptors in GHRH-positive neurons in the hypothalamus. This leads to selective stimulation of GH release from the pituitary. Unlike other GH secretagogues, ipamorelin stimulates GH release in a manner very similar to growth hormone releasing hormone (GHRH) without significantly affecting other hormonal axes.
In Vitro and In Vivo Activity
In primary rat pituitary cells, ipamorelin released GH with potency and efficacy comparable to GHRP-6 (EC₅₀ = 1.3 ± 0.4 nmol/l, Emax = 85 ± 5%).
In anaesthetised rats, ipamorelin released GH with ED₅₀ = 80 ± 42 nmol/kg and Emax = 1545 ± 250 ng GH/ml.
In conscious swine, ipamorelin released GH with ED₅₀ = 2.3 ± 0.03 nmol/kg and Emax = 65 ± 0.2 ng GH/ml plasma.
Induces longitudinal bone growth in rats and counteracts glucocorticoid‑induced decrease in bone formation.
Key Properties
Selective ghrelin receptor agonist – minimal off-target effects.
Stimulates GH release without significant effect on prolactin, cortisol, or other pituitary hormones.
High potency and efficacy in both in vitro and in vivo models.
Well‑characterised pentapeptide with defined sequence and high purity.
Synthetic, non‑natural amino acids (D‑2‑Nal, Aib) provide enhanced stability.
Applications
Endocrine research: Studies on GH secretion, pituitary function, and growth hormone regulation.
Bone metabolism: Investigating bone formation and glucocorticoid‑induced bone loss.
Metabolic research: Exploring nitrogen balance, protein metabolism, and catabolic states.
Aging and regenerative research: Studies on GH‑mediated tissue repair and regeneration.
Pharmacology: Evaluating ghrelin receptor agonists and their downstream effects.
Handling and Storage
Store lyophilized powder at –20°C in tightly sealed containers, protected from light and moisture.
After reconstitution, store at –80°C and avoid repeated freeze‑thaw cycles.
Reconstitute in sterile water, bacteriostatic water, or suitable buffer as required.
For research use only; not for human therapeutic or diagnostic use.
Use appropriate personal protective equipment (gloves, lab coat, safety goggles) when handling.
Quality Assurance
Each batch is tested for purity (by HPLC ≥98%), identity (by mass spectrometry), and sequence confirmation to ensure consistent quality.