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Phase IIVendors pendingFacts verified · 2026-05-25

Ipamorelin

Also known as nnc 26-0161, ipamorelin acetate · Wikipedia

Ipamorelin is a synthetic pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) classified as a selective ghrelin/GHSR1a receptor agonist. It was first described by Raun and colleagues at Novo Nordisk in 1998 as the first highly selective growth hormone secretagogue, distinguished from older GHRPs (GHRP-2, GHRP-6, hexarelin) by minimal elevation of cortisol, ACTH, prolactin, and aldosterone at GH-releasing doses. Helsinn advanced ipamorelin into Phase IIb trials for post-operative ileus, but the program was discontinued in 2014 after failure to meet endpoints. It is not FDA-approved for any indication and is sold as a research chemical and via US compounding pharmacies. Also known as: NNC 26-0161; ipamorelin acetate.

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Mechanism of action

Ipamorelin is the synthetic pentapeptide Aib-His-D-2-Nal-D-Phe-Lys-NH2 and a selective agonist of the growth hormone secretagogue receptor type 1a (GHSR1a), the endogenous ghrelin receptor on pituitary somatotrophs and hypothalamic neurons [Raun 1998 Eur J Endocrinol, PMID 9849822]. Receptor engagement triggers Gq/PLC-driven IP3 generation and intracellular Ca2+ release, evoking pulsatile release of stored growth hormone.

Ipamorelin is the synthetic pentapeptide Aib-His-D-2-Nal-D-Phe-Lys-NH2 and a selective agonist of the growth hormone secretagogue receptor type 1a (GHSR1a), the endogenous ghrelin receptor on pituitary somatotrophs and hypothalamic neurons [Raun 1998 Eur J Endocrinol, PMID 9849822]. Receptor engagement triggers Gq/PLC-driven IP3 generation and intracellular Ca2+ release, evoking pulsatile release of stored growth hormone. Unlike earlier GHRPs, ipamorelin does not appreciably elevate ACTH, cortisol, prolactin, or aldosterone at GH-active doses, and has weaker central orexigenic effects than ghrelin itself [Raun 1998]. Synergy with GHRH analogs (sermorelin, CJC-1295, tesamorelin) reflects complementary GHRHR + GHSR1a pathways converging on somatotroph GH exocytosis.

Pharmacokinetic properties

Half-life

~2 hours subcutaneous

Routes

subcutaneous · intramuscular

Bioavailability

Short-acting; commonly dosed multiple times daily or combined with a GHRH analog for synergy.

Amino-acid sequence

Aib-His-D-2-Nal-D-Phe-Lys-NH2

Use & research dosing

GH ReleaseMuscle GrowthSleep ImprovementSleep Quality

No FDA-approved dose exists (research framing only). The historic Helsinn Phase II post-operative ileus program used IV doses of approximately 0.03-0.3 mg/kg. Self-experimentation and compounded research protocols commonly use 100-300 mcg subcutaneously, 1-3 times daily (e.g., pre-bed and pre-workout), typically in 4-12 week cycles. Co-administration with a GHRH analog such as mod-GRF/CJC-1295 (no-DAC) at the same dose is the most common stacking pattern reported in the research-chemical literature.

Research-use framing only. SavePeptides sells nothing for human consumption. Doses above reflect reported research / self-experimentation ranges, not clinical recommendations.

Editorial perspective

Ipamorelin remains the cleanest and most selective GHSR1a/ghrelin-receptor agonist available, which is why it dominates modern GHRP+GHRH research stacks. Helsinn's Phase IIb post-operative ileus program (2014) was the highest-stage development effort and failed to meet endpoints, ending commercial drug-development interest. Despite this, the clean pharmacology profile keeps it widely used in research and compounding settings as the GHSR-side counterpart to sermorelin, CJC-1295, or tesamorelin.

— SavePeptides editorial desk · last updated 2026-05-25

Cautions & contraindications

Before researching this compound, note:

  • not FDA-approved for any indication; Helsinn Phase IIb program discontinued 2014
  • avoid in active or suspected malignancy (potential GH/IGF-1 axis stimulation)
  • avoid in pregnancy and breastfeeding
  • transient lightheadedness, head rush, and injection-site irritation are common
  • may cause mild fluid retention and peripheral edema
  • may impair insulin sensitivity with chronic use
  • co-administration with somatostatin analogs (octreotide, lanreotide) blunts GH response
  • compounded purity and identity vary widely outside GMP supply

Research foundation

The papers behind the page.

  1. [01]https://pubmed.ncbi.nlm.nih.gov/9849822/
  2. [02]https://pubmed.ncbi.nlm.nih.gov/19289567/
  3. [03]https://pubmed.ncbi.nlm.nih.gov/12168778/

Facts verified

2026-05-25

Confidence

medium

What this means

  • Helsinn Phase IIb discontinued 2014 — no marketed approval anywhere

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