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GH Secretagogue

Ipamorelin

NNC 26-0161 · Ipamorelin acetate

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Mechanism of Action

Ipamorelin is a synthetic pentapeptide and selective growth hormone secretagogue receptor (GHS-R1a) agonist. Its sequence is Aib-His-D-2-Nal-D-Phe-Lys-NH₂. Unlike earlier GHRPs (GHRP-2, GHRP-6), ipamorelin is highly selective for GHS-R1a without elevating ACTH, cortisol, prolactin, or aldosterone at therapeutic doses — the most common reason it is preferred over non-selective GHRPs. It stimulates pulsatile growth hormone release from pituitary somatotropes through the ghrelin receptor pathway, distinct from the GHRH receptor pathway that sermorelin and CJC-1295 engage. This complementarity is why ipamorelin is most commonly stacked with CJC-1295: the GHRH analogue amplifies the GH pulse amplitude while ipamorelin amplifies pulse frequency via a different receptor, producing an additive secretagogue effect documented in the Teichman 2006 phase I/II trial.

Research Notes
Selective GHS-R1a agonism without ACTH, cortisol, or prolactin elevation — confirmed in human pharmacology studies
Pulsatile GH release: preserves natural GH secretion rhythm (unlike continuous exogenous HGH)
Stacked with CJC-1295 DAC: Teichman 2006 showed 2–10× GH elevation sustained for 9–11 days
Improved body composition: lean mass gain, fat mass reduction in GH secretagogue literature
Sleep quality improvement: GH secretion peaks during slow-wave sleep, enhanced by ipamorelin protocols
Shorter half-life (~2 hours) allows dosing flexibility and rapid clearance vs long-acting alternatives
Extended Research Notes

Teichman et al. (JCEM, 2006; PubMed 16352683) remains the definitive human pharmacology study: CJC-1295 (with DAC) in 57 healthy adults produced 2–10× GH elevation and 1.5–3× IGF-1 elevation sustained for 9–11 days. Ipamorelin was studied alongside as a GHS-R1a component. The combination produces additive effects through dual receptor engagement. Human data for ipamorelin specifically (without the CJC stack) is limited. Both compounds removed from FDA Category 2 September 2024; WADA prohibits both in sport.

Full Profile Reference

IpamorelinAlso known as: NNC 26-0161, Ipamorelin acetate

Mechanism of Action

Ipamorelin is a synthetic pentapeptide and selective growth hormone secretagogue receptor (GHS-R1a) agonist. Its sequence is Aib-His-D-2-Nal-D-Phe-Lys-NH₂. Unlike earlier GHRPs (GHRP-2, GHRP-6), ipamorelin is highly selective for GHS-R1a without elevating ACTH, cortisol, prolactin, or aldosterone at therapeutic doses — the most common reason it is preferred over non-selective GHRPs. It stimulates pulsatile growth hormone release from pituitary somatotropes through the ghrelin receptor pathway, distinct from the GHRH receptor pathway that sermorelin and CJC-1295 engage. This complementarity is why ipamorelin is most commonly stacked with CJC-1295: the GHRH analogue amplifies the GH pulse amplitude while ipamorelin amplifies pulse frequency via a different receptor, producing an additive secretagogue effect documented in the Teichman 2006 phase I/II trial.

Reported Research Benefits

  • Selective GHS-R1a agonism without ACTH, cortisol, or prolactin elevation — confirmed in human pharmacology studies
  • Pulsatile GH release: preserves natural GH secretion rhythm (unlike continuous exogenous HGH)
  • Stacked with CJC-1295 DAC: Teichman 2006 showed 2–10× GH elevation sustained for 9–11 days
  • Improved body composition: lean mass gain, fat mass reduction in GH secretagogue literature
  • Sleep quality improvement: GH secretion peaks during slow-wave sleep, enhanced by ipamorelin protocols
  • Shorter half-life (~2 hours) allows dosing flexibility and rapid clearance vs long-acting alternatives

Dosing Protocol & Reconstitution

Reported Research Dosing — Not Clinical Recommendations

Ipamorelin is most commonly dosed alongside CJC-1295 because the two peptides hit independent receptors (ghrelin and GHRH) and their GH-releasing effects add together. Monotherapy is reasonable for an initial cycle to establish tolerability.

Ipamorelin Monotherapy

DoseFrequencyTimingTypical Cycle
200 mcg1× dailyPre-bed4–6 weeks (first cycle)
200–300 mcg2–3× dailyWaking, post-workout, pre-bed8–12 weeks

The pre-bed dose is universally included because natural GH pulse is largest overnight, and ipamorelin compounds with the endogenous pulse.

Ipamorelin + CJC-1295 (non-DAC / Mod GRF 1-29) Stack

PeptideDoseFrequencyTiming
Ipamorelin200 mcg1–3× dailyFasted windows, pre-bed
CJC-1295 non-DAC100–200 mcg1–3× daily (same injections)Co-administered with ipamorelin

Both peptides have short half-lives (~2 hours and ~30 minutes respectively), so pulsatile dosing preserves pituitary responsiveness. The two are typically drawn into the same insulin syringe and injected together.

Ipamorelin + CJC-1295 DAC Stack

PeptideDoseFrequencyTiming
Ipamorelin200–300 mcg1× dailyPre-bed
CJC-1295 DAC1–2 mgOnce weeklyAny day

CJC-1295 DAC has a 6–8 day half-life via albumin binding. Weekly dosing produces sustained GHRH signalling (not pulsatile). This trades dosing convenience for loss of natural pulsatility — see the Ipamorelin vs CJC-1295 comparison for the pulsatile-vs-sustained trade-off.

Administration

  • Route: subcutaneous injection
  • Site rotation: abdomen, thigh — rotate
  • Timing principles:
    • Pre-bed dose aligns with natural nocturnal GH surge
    • Fasted state is preferred (carbohydrate/insulin spikes blunt GH response)
    • Space injections at least 3 hours from heavy meals

Reconstitution

Ipamorelin:

  • 5 mg vial + 2 mL bacteriostatic water = 2,500 mcg/mL (200 mcg per 0.08 mL on U-100 insulin syringe = 8 units).

CJC-1295 (non-DAC or DAC):

  • 5 mg vial + 2 mL bacteriostatic water = 2,500 mcg/mL (100 mcg per 0.04 mL = 4 units on U-100).

Both store refrigerated at 2–8°C after reconstitution. Stable for 28 days. Do not freeze.

Cycle Duration and Monitoring

  • Typical cycle: 12–24 weeks
  • Monitoring: baseline and 10–12 week IGF-1 measurement is the most common biomarker
  • Washout: 4–8 weeks between cycles is standard practitioner practice

Contraindications

  • Active malignancy — GH/IGF-1 axis elevation is a theoretical oncogenic concern
  • Diabetes mellitus — GH elevates insulin resistance; monitor glucose
  • Cardiovascular disease — sustained IGF-1 elevation has unclear long-term cardiac implications
  • Pregnancy and lactation — no data; avoid
  • Pediatric use — not indicated outside controlled GH-deficiency treatment

Regulatory Status (as of April 2026)

Both ipamorelin and CJC-1295 were removed from the FDA Section 503A bulks list in September 2024, restricting compounding-pharmacy access. Current status remains research-compound in most jurisdictions. WADA prohibits both in competitive sport.

Research Notes

Teichman et al. (JCEM, 2006; PubMed 16352683) remains the definitive human pharmacology study: CJC-1295 (with DAC) in 57 healthy adults produced 2–10× GH elevation and 1.5–3× IGF-1 elevation sustained for 9–11 days. Ipamorelin was studied alongside as a GHS-R1a component. The combination produces additive effects through dual receptor engagement. Human data for ipamorelin specifically (without the CJC stack) is limited. Both compounds removed from FDA Category 2 September 2024; WADA prohibits both in sport.

Research Summary

Teichman et al. (JCEM 2006) phase I/II human data: CJC-1295 produced 2–10× GH and 1.5–3× IGF-1 elevation for 9–11 days. Ipamorelin as selective GHRP lacks cortisol/ACTH activation. Both compounds FDA Category 2 as of September 2024 (removed from compounding list). Reclassification to Category 1 expected under RFK/HHS review. WADA prohibited.

Side Effects & Safety

Reported in clinical series (injection-based protocols): injection site reactions (mild erythema, most common), transient headache, mild fluid retention at initiation. GH-class effects at higher doses: increased hunger, mild joint aches (water retention), transient insulin resistance — monitor fasting glucose. No ACTH, cortisol, or prolactin elevation at therapeutic doses (key selectivity advantage over GHRP-2/GHRP-6). Long-term safety data (>1 year) not available from published RCTs. WADA prohibited.

Stability & Storage

Lyophilised powder: stable at -20°C for 2–3 years. After reconstitution with bacteriostatic water: store at 4°C, use within 21–28 days. Sensitive to repeated freeze-thaw cycles.

Molecular Data

Sequence
Aib-His-D-2-Nal-D-Phe-Lys-NH₂ (Aib = α-aminoisobutyric acid; D-2-Nal = D-2-naphthylalanine)
Molecular Formula
C38H49N9O5
Molecular Weight
711.9 Da
CAS Number
170851-70-4
Half-Life
~2 hours (subcutaneous)

Primary literature: https://pubmed.ncbi.nlm.nih.gov/16352683/