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Ipamorelin

Technical Monograph

Ipamorelin is a synthetic pentapeptide and a potent, selective growth hormone secretagogue (GHS) and ghrelin receptor agonist. It is structurally distinct from other GHRPs, designed to stimulate significant growth hormone release from the anterior pituitary without inducing simultaneous elevations in cortisol, ACTH, or prolactin, ensuring an isolative profile of GH secretion.

Mechanism of Action

Ipamorelin acts as a mimetic of ghrelin, binding with high selectivity to the growth hormone secretagogue receptor 1a (GHSR-1a). Activation initiates a signal transduction cascade dependent on phospholipase C, generating inositol triphosphate (IP3) and leading to intracellular calcium mobilization. This triggers the exocytotic release of stored growth hormone from somatotropes.

Pharmacological Detail

Selective GHSR-1a agonist activating the PLC/IP3/Ca2+ intracellular pathway exclusively in pituitary somatotropes.

Pharmacodynamics

Induces robust, pulsatile exocytosis of growth hormone. Sustains elevated IGF-1 output from the liver secondary to GH action.

Pharmacokinetics

High systemic bioavailability via parenteral administration. Exhibits a terminal half-life of approximately 120 minutes in in-vivo models.

Preclinical Observations & In Vitro Data

Extensive preclinical data confirms high safety margins and unique selectivity for GH release. Models demonstrate significant increases in body weight gain and longitudinal bone growth without corresponding shifts in stress hormones.

Preclinical (Rat): Dose-dependent stimulation of longitudinal bone growth velocity. GH peaks matching maximal physiological amplitudes.
In Vitro (Pituitary Cells): EC50 of 1.3 ± 0.4 nM for GH release. Complete absence of ACTH or PRL release.

Observed Timeline of Action

TimeframePharmacological Effect
20-40 minsPeak plasma circulating GH concentrations.
120 minsClearance phase initiation; terminal half-life boundary.
Days 14-21Stable, elevated systemic circulating IGF-1 profiles in sustained models.

Abstract Highlights

  • Demonstrates highly selective GH secretion without prolactin or cortisol elevation
  • Exhibits dose-dependent efficacy in stimulating long bone growth in preclinical models
  • Preserves normal pulsatile pattern of endogenous GH release
  • Shows prolonged half-life (approx. 2 hours) relative to synthetic GHRP-6

References

Raun K, et al. (1998)."Ipamorelin, the first selective growth hormone secretagogue."European Journal of Endocrinology.

Chemical Specifications

711.86 g/mol
C38H49N9O5
Aib-His-D-2Nal-D-Phe-Lys-NH2

Material Handling & Stability

Laboratory StorageLyophilized powder: Store at -20°C to -80°C.
Aqueous StabilityReconstituted: Maintain at 2-8°C. Stable for 21-28 days with bacteriostatic agents.

Strict Notice

THIS COMPOUND IS PRODUCED FOR LABORATORY RESEARCH PURPOSES ONLY. NOT FOR HUMAN CONSUMPTION. MATERIAL DATA SHEETS AND LABORATORY GUIDELINES SHOULD BE CONSULTED PRIOR TO HANDLING.