Ipamorelin molecular structure
Ipamorelin molecular structure
Clinical Trial
📈Growth Hormone

Ipamorelin

Also known as: IPA, NNC 26-0161, NNC-26-0161, IPAM

MW

711.85 Da

Formula

C38H49N9O5

CAS

170851-70-4

Routes

2 routes

Ipamorelin is a synthetic pentapeptide growth hormone secretagogue (GHS) that selectively stimulates growth hormone (GH) release from the anterior pituitary gland by acting as an agonist at the ghrelin/growth hormone secretagogue receptor (GHS-R1a). Developed by Novo Nordisk in the late 1990s, it is considered one of the most selective GH secretagogues available, distinguished by its clean pharmacological profile with minimal effects on cortisol, prolactin, and appetite. Unlike earlier growth hormone secretagogues such as GHRP-6 and GHRP-2, ipamorelin does not significantly stimulate ACTH, cortisol, or prolactin release at GH-stimulating doses — a selectivity that results from its specific binding characteristics at the GHS-R1a receptor. It produces a dose-dependent, pulsatile release of growth hormone that closely mimics the physiological GH secretion pattern. Ipamorelin has undergone Phase 2 clinical trials for post-operative ileus recovery and continues to be researched for applications in age-related GH decline, body composition improvement, and recovery from injury. It is frequently combined with GHRH analogs (CJC-1295, Mod GRF 1-29) for synergistic GH release.

Research Use OnlyFor educational and research purposes only

Research Applications

Age-Related GH Decline (Somatopause)

Ipamorelin research focuses on restoring youthful GH pulsatility in aging adults. Studies demonstrate significant increases in GH pulse amplitude and IGF-1 levels without disrupting circadian GH rhythms. Its clean side effect profile makes it particularly suitable for this application.

Post-Operative Recovery

Phase 2 clinical trials evaluated ipamorelin for post-operative ileus (delayed bowel function recovery). Results showed accelerated return of bowel function and reduced hospital stay following abdominal surgery, with improvements in gastric motility and intestinal transit time.

Body Composition Improvement

Research demonstrates ipamorelin-stimulated GH release promotes lean body mass accretion and visceral fat reduction. Combined with GHRH analogs, studies show improvements in lean mass, fat mass, and body composition parameters in both animal models and human subjects.

Bone Density Enhancement

GH and IGF-1 are critical regulators of bone metabolism. Ipamorelin research shows increased bone mineral density and improved bone formation markers (osteocalcin, P1NP) in preclinical models, suggesting potential applications in osteoporosis prevention and fracture healing.

Sleep Quality and Recovery

GH release is closely linked to slow-wave sleep. Ipamorelin administered before bedtime has been studied for enhancing sleep-related GH pulses, improving sleep quality metrics, and accelerating recovery from physical exertion.

Muscle Injury Recovery

Preclinical studies demonstrate accelerated skeletal muscle regeneration following injury, with increased satellite cell activation, myofiber protein synthesis, and faster functional recovery — mediated through IGF-1-dependent mechanisms.

Mechanism of Action

GHS-R1a Receptor Activation

Ipamorelin binds to the growth hormone secretagogue receptor type 1a (GHS-R1a), a G-protein coupled receptor primarily expressed on somatotroph cells of the anterior pituitary. Receptor activation stimulates the Gq/11 signaling cascade, leading to phospholipase C activation, IP3-mediated calcium release from intracellular stores, and subsequent growth hormone vesicle exocytosis.

Selective GH Release

Ipamorelin's selectivity stems from its specific receptor binding profile — it activates GHS-R1a at the pituitary with high potency but has minimal activity at other receptor subtypes involved in ACTH/cortisol release. Studies demonstrate that even at doses 100-fold above the GH-stimulating dose, ipamorelin does not significantly increase cortisol or ACTH levels — a unique feature among GH secretagogues.

Pulsatile Secretion Pattern

Unlike exogenous growth hormone administration (which produces sustained supraphysiological levels), ipamorelin stimulates pulsatile GH release that preserves the natural rhythm of GH secretion. This pulsatile pattern maintains GH receptor sensitivity and downstream IGF-1 signaling without the receptor desensitization seen with continuous GH exposure.

Synergy with GHRH

Ipamorelin works synergistically with growth hormone releasing hormone (GHRH) and its analogs. While GHRH activates GH synthesis and the cAMP/PKA pathway in somatotrophs, ipamorelin releases stored GH through the calcium/IP3 pathway. Combined administration produces GH release greater than the sum of individual effects.

Somatostatin Functional Antagonism

Ipamorelin partially antagonizes the inhibitory effect of somatostatin on GH release, allowing for GH secretion even during periods of high somatostatin tone. This contributes to more consistent GH stimulation across different physiological states.

Biological Pathways

Gq/11-PLC-IP3/DAG Pathway

GHS-R1a activation couples to Gq/11 proteins, activating phospholipase C (PLC). PLC cleaves PIP2 into IP3 and DAG. IP3 triggers calcium release from the endoplasmic reticulum, while DAG activates protein kinase C (PKC). The resulting calcium surge triggers GH granule exocytosis from somatotroph cells.

GH/IGF-1 Axis

Released GH activates the JAK2/STAT5 signaling pathway in hepatocytes, stimulating hepatic IGF-1 synthesis. Circulating IGF-1 acts through the IGF-1 receptor (a receptor tyrosine kinase) to activate PI3K/Akt and MAPK/ERK pathways in target tissues, promoting protein synthesis, cell proliferation, and metabolic effects.

mTOR/p70S6K Protein Synthesis

GH and IGF-1 signaling converge on the mTOR pathway, activating p70S6K and 4E-BP1 to enhance ribosomal protein synthesis. This is the primary mechanism through which ipamorelin-stimulated GH release promotes muscle protein accretion and tissue repair.

Lipolytic Pathway

GH activates hormone-sensitive lipase (HSL) in adipocytes through a JAK2-mediated mechanism independent of IGF-1, directly stimulating lipolysis. This GH-mediated fat mobilization contributes to improved body composition with favorable fat-to-muscle ratios.

Dosage Information

Typical dosage ranges for research applications. Always verify with current literature.
Typical Dose
300 mcg
Dose Range
200 - 500 mcg
Frequency
1-3 times daily on empty stomach, before bedtime preferred
Dosage Calculator
Calculate precise peptide dosages based on your reconstitution parameters
Dosage calculation parameters
Vial size in milligrams
Reconstitution volume in milliliters
Body weight input
Recommended dose per kg
mcg/kg
Desired dose input
mcg

Calculation Results

Concentration
2.5 mg/ml
Dose Volume
0.1 ml0.100 ml
Insulin Syringe
10 units
Doses per Vial
2020 doses @ 250 mcg

Syringe Fill Level (100u syringe)

05010010.0uunits
0u10.0 / 100 units (10%)100u

Protocols

CJC-1295 + Ipamorelin Stack
Intermediate
🏃Sport & Performance
3-6 months

The most popular GH secretagogue stack. Synergistic effects for fat loss, muscle gain, recovery, and anti-aging.

Dosage
CJC-1295: 200-300mcg, Ipamorelin: 200-300mcg
Frequency
Once daily before bedtime on empty stomach. 5 days on, 2 days off.
Cycle
5 days on, 2 days off weekly. 3-6 month cycles, then 1 month off.
Stacking Notes
Inject both peptides together SubQ. Best results when combined with proper sleep (8+ hours) and resistance training. Can add MK-0677 for additional GH boost.

Warning: May increase hunger. Water retention possible. Monitor for numbness/tingling.

Comprehensive Longevity Stack
Advanced
Anti-Aging
3-6 months

Multi-peptide anti-aging protocol combining telomerase activation, mitochondrial support, and GH optimization.

Dosage
Epithalon: 1mg daily, MOTS-c: 10mg 2x/week, NAD+: 500mg daily, CJC/Ipa: 200mcg each daily
Frequency
Daily or as specified per peptide
Cycle
Epithalon: 50-day course yearly. MOTS-c: Ongoing 2x/week. NAD+: Daily. CJC/Ipa: 5 on/2 off.
Stacking Notes
Comprehensive approach targeting multiple aging pathways. Requires significant commitment and cost.

Warning: Very advanced protocol. Consider blood work monitoring.

Stability & Storage

Ipamorelin is supplied as a lyophilized white powder. Store lyophilized form at -20°C for long-term stability (18-24 months). At 2-8°C, the powder remains stable for approximately 3-6 months. Protect from light, heat, and moisture.

Reconstitute with bacteriostatic water (0.9% benzyl alcohol preserved) by directing the water stream down the inner wall of the vial. Allow to dissolve gently without shaking. The resulting solution should be clear and colorless. Any cloudiness or particulate matter indicates degradation.

Reconstituted ipamorelin should be stored at 2-8°C and used within 21-28 days. Do not freeze reconstituted solution. The peptide is stable at pH 4-7 but degrades more rapidly at alkaline pH. Avoid mixing with other peptides in the same vial unless compatibility is verified — combination with CJC-1295 or Mod GRF 1-29 in the same vial is commonly practiced but may slightly reduce stability.

Side Effects & Precautions

Injection Site Reactions

Mild redness, swelling, or itching at the injection site is common and typically self-limiting. Rotating injection sites reduces local irritation.

Head Rush and Headache

Transient lightheadedness or mild headache following injection has been reported, possibly related to transient changes in blood glucose or growth hormone effects on cerebral vasculature. Usually resolves within 30-60 minutes.

Water Retention

Mild fluid retention (edema in hands and feet) may occur, particularly during the initial weeks of use. This is a class effect of GH stimulation and typically resolves with continued use as the body adjusts.

Numbness and Tingling

Carpal tunnel-like symptoms (numbness, tingling in hands) can occur due to GH-mediated fluid retention affecting the median nerve. This is dose-dependent and resolves with dose reduction.

Hunger Stimulation

While ipamorelin is significantly less orexigenic than GHRP-6, mild increases in appetite have been reported by some users, likely mediated through residual GHS-R1a activation in hypothalamic feeding centers.

Cortisol and Prolactin (Minimal)

Unlike GHRP-2 and GHRP-6, ipamorelin does not significantly elevate cortisol or prolactin at standard GH-stimulating doses. This selectivity is a key safety advantage over other GH secretagogues.

Research Use Only. This information is for educational and research purposes only. Not intended for medical advice or self-medication.

Regulatory Status

Clinical Trial

Ipamorelin is not approved by the FDA or any major regulatory authority for clinical use. It has an Investigational New Drug (IND) status and has completed Phase 2 clinical trials for post-operative ileus, but development was not continued to Phase 3.

The peptide is classified as a research chemical and is available from peptide synthesis companies for laboratory research purposes. It is not approved for human therapeutic use in any country.

WADA prohibits ipamorelin under category S2 (Peptide Hormones, Growth Factors, Related Substances, and Mimetics) of the prohibited list, banned both in-competition and out-of-competition. Detection methods using LC-MS/MS can identify ipamorelin and its metabolites in urine for several days after administration.

Research Studies

Ipamorelin, a New Growth-Hormone-Releasing Peptide, Induces Growth Hormone Release Selectively

Raun K, Hansen BS, Johansen NL, et al.

Journal of Endocrinology
1998
View Source

Ipamorelin, a Novel Ghrelin Mimetic, Does Not Release Cortisol or ACTH

Johansen PB, Nowak J, Skjaerbaek C, et al.

Biochemical and Biophysical Research Communications
1999
View Source

Phase 2 Study of Ipamorelin for Post-operative Ileus

Beck DE, Sweeney WB, McCarter MD, et al.

Diseases of the Colon and Rectum
2008
View Source

Growth Hormone Secretagogues: History, Mechanism of Action, and Clinical Applications

Ghigo E, Arvat E, Muccioli G, et al.

Annales d'Endocrinologie
2002
View Source

Selectivity of Ipamorelin as a Growth Hormone Secretagogue

Hansen BS, Raun K, Nielsen KK, et al.

European Journal of Endocrinology
1999
View Source
Dosage Calculator
Calculate reconstitution volumes and injection amounts for Ipamorelin.
Explore More
Explore more peptides in the Growth Hormone category and related research.