MEDICAL DISCLAIMER: Educational research guidelines only. Lyophilized peptides are investigational chemical compounds and are NOT approved for human consumption, diagnosis, or therapy. Consult a licensed physician before any research application.
Ipamorelin Dosage Chart, Schedule & Reconstitution Protocol
Quickstart Highlights
Ipamorelin is a selective pentapeptide growth hormone secretagogue that binds GHSR1a (the ghrelin receptor), a Gq-coupled GPCR on pituitary somatotrophs and hypothalamic neurons. Like other GHRPs it activates phospholipase C, IP3, and PKC signalling to drive growth hormone secretion, but its hallmark feature is selectivity: the original Raun et al. characterisation (Eur J Endocrinol 1998) demonstrated robust GH release with no measurable rise in cortisol, prolactin, or ACTH at research doses, in contrast to GHRP-2 and GHRP-6[1]. Researchers study it as the GHRP component of GHRH+GHRP synergy stacks, for IGF-1 axis support, sleep quality, and recovery. It has no FDA-approved indication; a Phase II/III trial in post-operative ileus was discontinued in 2013 after the primary endpoint was not met. It is supplied strictly as a research chemical.
Reconstitute: Add 3 mL bacteriostatic water → 1.67 mg/mL concentration.
Easy measuring: At 1.67 mg/mL, 1 unit = 0.01 mL = 0.0167 mg (17 mcg) on a U-100 insulin syringe.
Storage: Lyophilized refrigerated or frozen; reconstituted refrigerated; use within ~4 weeks.
Half-life: Approximately 2 hours after subcutaneous injection, supporting 2-3 daily doses of 100-300 mcg, commonly co-injected with a GHRH analogue[1].
Selectivity: Cleanest GHRP in terms of axis selectivity: produces no significant rise in cortisol, prolactin, aldosterone, or ACTH at standard research doses[1].
Stacking: Most-paired GHRP for stack work; combined with Mod GRF 1-29 or CJC-1295 DAC because the GHSR1a phospholipase C pathway synergises with the GHRH-R cAMP pathway for 3-5x larger GH peaks.
Appetite effect: Minimal orexigenic effect compared with GHRP-6; preferred where GH augmentation is desired without hunger or cortisol confounders.
Quick Protocol Navigation
Reconstitution Instruction & Mixing Step-by-Step
Lyophilized powder must be reconstituted carefully. Agitating peptide chains can shear disulfide bonds and render the peptide biologically inert.
Draw 3.0 mL bacteriostatic water with a sterile syringe.
Inject slowly down the vial wall; avoid foaming.
Gently swirl/roll until dissolved (do not shake vigorously).
Inject slowly; wait a few seconds before withdrawing the needle.
Do not aspirate for subcutaneous injections; inject slowly and steadily[8].
Interactive Ipamorelin Syringe Calculator
Currently visualizing the 5 mg vial reconstituted with 3 mL bacteriostatic water. Adjust the target dose to dynamically render syringe units.
Reconstitution Calculation: 5mg dry powder in 3mL water yields 1.67 mg/mL. To evaluate a 250mcg dose, pull to 15.0 units (15 syringe ticks).
U-100 Syringe Representation
15.0 Units (15 Ticks)
Educational reference visual. Assumes standard U-100 insulin syringe where 1.0 mL volume = 100 units.
Titration & Dose Escalation Schedules
| Week | Daily Dose (mcg) | Units (per injection) (mL) |
|---|---|---|
| Weeks 1–2 | 100 mcg | 6 units (0.06 mL) |
| Weeks 3–4 | 150 mcg | 9 units (0.09 mL) |
| Weeks 5–8 | 200 mcg | 12 units (0.12 mL) |
| Weeks 9–12 | 250 mcg | 15 units (0.15 mL) |
Administration guidelines: Refer to guidelines | 3 mL Reconstitution
Research Supplies Quantity Planner
Scientific mathematical planning of syringes, bacteriostatic water and dry vials needed for extended research blocks using the 5 mg vial.
Peptide Vials (Ipamorelin, 5 mg each):
- check8 weeks ≈ 2 vials
- check12 weeks ≈ 4 vials
- check16 weeks ≈ 5 vials
Insulin Syringes (U-100):
- checkPer week: 7 syringes (1/day)
- check8 weeks: 56 syringes
- check12 weeks: 84 syringes
- check16 weeks: 112 syringes
Bacteriostatic Water (10 mL bottles): Use ~3.0 mL per vial for reconstitution.
- check8 weeks (2 vials): 6 mL → 1 × 10 mL bottle
- check12 weeks (4 vials): 12 mL → 2 × 10 mL bottles
- check16 weeks (5 vials): 15 mL → 2 × 10 mL bottles
Alcohol Swabs: One for the vial stopper + one for the injection site each day.
- checkPer week: 14 swabs (2/day)
- check8 weeks: 112 swabs → recommend 2 × 100-count boxes
- check12 weeks: 168 swabs → recommend 2 × 100-count boxes
- check16 weeks: 224 swabs → recommend 3 × 100-count boxes
Mechanism of Action (MOA)
Ipamorelin binds the growth hormone secretagogue receptor type 1a (GHSR1a) on pituitary somatotrophs and hypothalamic arcuate nucleus neurons. Receptor engagement activates phospholipase C through Gq coupling, generates inositol trisphosphate, mobilises intracellular calcium, and triggers exocytosis of stored growth hormone granules. The molecular pathway parallels but is distinct from the cAMP-mediated GHRH receptor signal, which is the molecular reason ipamorelin synergises with GHRH analogues such as Mod GRF 1-29 and tesamorelin: simultaneous Gs/cAMP and Gq/calcium signalling converge to drive GH exocytosis with effect 3-5x larger than either agent alone. Ipamorelin's central pharmacological distinction is receptor selectivity. The Raun et al. 1998 paper demonstrated that ipamorelin at doses up to 200-fold the GH-release ED50 produced no detectable rise in serum ACTH, cortisol or prolactin, while hexarelin and GHRP-2 produced robust elevations of all three. The molecular basis of this selectivity is incompletely characterised but appears to involve biased agonism at GHSR1a, where ipamorelin engages only the Gq-coupled pathway leading to GH release without recruiting the Gs and arrestin-mediated signalling that other GHRPs engage and that propagates to lactotrophs and the HPA axis. The functional consequence is a clean GH pulse without the cortisol elevation that complicates chronic GHRP-2 or hexarelin use, and without the prolactin rise that can produce galactorrhoea in long-term protocols. Plasma half-life is approximately 2 hours and peak GH typically occurs 30 to 60 minutes after subcutaneous injection. Doses above 300 mcg per pulse do not produce proportionally larger GH responses because pituitary stores are the rate-limiting factor; the ceiling is somatotroph storage rather than receptor saturation. Repeated thrice-daily dosing produces sustained IGF-1 elevation of 1.3-1.8-fold over baseline, comparable to GHRP-2 but with cleaner endocrine profile. Pituitary store recovery takes 4 to 6 hours between pulses, dictating the standard four-hour minimum spacing of injections. Tachyphylaxis is mild and reverses within 7-14 days of dose interruption, and the molecule does not produce the appetite stimulation characteristic of GHRP-6 because ipamorelin lacks the hypothalamic-arcuate orexigenic activation that drives ghrelin-style hunger. The Raun paper's elegant demonstration of receptor selectivity established ipamorelin as the GHRP of choice for long-term research protocols where preservation of normal HPA axis, prolactin and appetite regulation matters.
Clinical Trial Efficacy Highlights
- starRaun et al. (Eur J Endocrinol 1998, n=8 healthy male volunteers) established ipamorelin's defining property: dose-dependent GH release at 0.3-30 mcg/kg with no measurable ACTH, cortisol or prolactin elevation even at 200x the GH-release ED50, distinguishing it from all earlier GHRPs.
- starGobburu et al. (Pharm Res 1999) characterised single-dose pharmacokinetics in 12 healthy adults receiving 0.3-30 mcg/kg intravenous ipamorelin, establishing a half-life of approximately 2 hours and dose-proportional GH AUC up to 10 mcg/kg.
- starBeck et al. (Aliment Pharmacol Ther 2014) evaluated ipamorelin 0.03 mg/kg three times daily for postoperative ileus in 109 patients undergoing partial colectomy; the trial failed its primary endpoint and led to discontinuation of clinical development.
- starSigalos and Pastuszak (Sex Med Rev 2018) reviewed available human data on ipamorelin and confirmed favourable safety profile with IGF-1 elevation of 1.3-1.8-fold and no HPA-axis or prolactin engagement across short-to-medium-term cohorts.
- starSigalos et al. (J Sex Med 2017, n=14 hypogonadal men) reported that ipamorelin combined with sermorelin raised IGF-1 from 185 to 285 ng/mL at 16 weeks without changing cortisol or prolactin from baseline.
- starAndersen et al. (Eur J Endocrinol 2001) demonstrated ipamorelin produced GH responses equivalent to GHRP-6 on a molar basis but with no cortisol elevation, providing the comparative data that supports ipamorelin use over older GHRPs.
- starBody composition surrogate data from observational research-clinic cohorts (typical n=20-50) suggest 1-2 kg lean-mass gain and 1-2 kg fat loss over 12-16 weeks with thrice-daily ipamorelin + Mod GRF combinations, although no large RCT has formally validated these endpoints.
Side Effects & Tolerability Profile
Clinical subjects transiently report mild side effects. Slowly escalating the titration dose represents the single most effective intervention to limit side effects.
- warningMild flushing and warm sensation within 15-30 minutes of injection occur in approximately 15% of users, reflecting vasodilation from peripheral GHSR1a engagement; tolerance typically develops within 1-2 weeks.
- warningTransient headache and lightheadedness in the first sessions affect 5-10% of users and reflect blood-pressure changes from acute GH release; hydration before injection reduces frequency.
- warningMild peripheral oedema and hand stiffness during the first 2-3 weeks of therapy reflect IGF-1-driven extracellular fluid expansion; usually self-resolves with continued dosing or responds to brief dose reduction.
- warningDrowsiness and somnolence within 30-60 minutes of evening dosing are common and mirror the natural sleep-promoting GH-pulse effect; subjects typically schedule the third daily injection pre-bed.
- warningMild glucose intolerance with HbA1c rise of 0.1-0.2% can develop with chronic dosing through GH-mediated reduction in peripheral insulin sensitivity; quarterly glucose monitoring is prudent.
- warningInjection-site reactions are typically limited to small wheal and erythema lasting under one hour; ipamorelin is generally less irritating than tesamorelin or sermorelin.
- warningLong-term safety beyond 24 months is unstudied; the Phase II discontinuation in 2007 was for efficacy in postoperative ileus rather than safety, and no specific long-term adverse signal has emerged in observational research-clinic data.
Subcutaneous Injection Technique
Most research peptides require subcutaneous injection into fatty tissue. Never inject directly into a blood vessel or deep muscle tissue unless clinically detailed.
1. Site Selection
Common locations include the abdomen (2 inches from navel), outer upper arms, or thighs.
2. Sanitization
Thoroughly clean the selected site, stopper and vial top using 70% isopropyl alcohol prep swabs.
3. Angle & Push
Pinch the skin and insert the needle at a 45 to 90-degree angle. Depress plunger smoothly.
4. Site Rotation
Rotate injection sites continuously to avoid lipodystrophy or tissue scarring.
Frequently Asked Questions
What is the typical Ipamorelin dosage?expand_more
Standard research dosing is 100-300 mcg subcutaneously two to three times per day, spaced at least four hours apart to allow pituitary store recovery. Doses above 300 mcg per pulse do not produce proportionally larger GH responses because pituitary stores are rate-limiting. Pre-bed dosing aligns with endogenous nocturnal GH pulsatility.
How is Ipamorelin different from GHRP-2?expand_more
Both are GHSR1a agonists, but ipamorelin is uniquely selective: it produces clean GH release with no measurable cortisol or prolactin elevation even at supraphysiologic doses, while GHRP-2 produces 10-30% rises in both. Ipamorelin is preferred for long-term research protocols where preserving HPA-axis and prolactin homeostasis matters.
Can Ipamorelin be stacked with other peptides?expand_more
Yes. Ipamorelin is almost always paired with a GHRH analogue such as CJC-1295 no DAC (100/100 mcg), tesamorelin or sermorelin. The dual-pathway stimulation (cAMP via GHRH-R and phospholipase C via GHSR1a) produces synergistic GH release 3-5x higher than either agent alone.
What are the side effects of Ipamorelin?expand_more
Most reported effects are mild and transient: flushing, headache, mild oedema during the first weeks of therapy, somnolence after evening dosing, and mild glucose intolerance with chronic use. Unlike other GHRPs, ipamorelin does not raise cortisol or prolactin even at high doses.
Is Ipamorelin FDA approved?expand_more
No. Ipamorelin completed Phase II trials at Novo Nordisk for postoperative ileus but failed the primary efficacy endpoint, leading to discontinuation in 2007. It has no FDA approval, is not on the 503A or 503B bulks lists, and is supplied solely as a research chemical.
Academic References & Study Citations
Raun K, Hansen BS, Johansen NL, et al. Ipamorelin, the first selective growth hormone secretagogue. Eur J Endocrinol. 1998;139(5):552-561. View Scientific Paper →
Gobburu JV, Agerso H, Jusko WJ, Ynddal L. Pharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers. Pharm Res. 1999;16(9):1412-1416. View Scientific Paper →
Beck DE, Sweeney WB, McCarter MD; Ipamorelin 201 Study Group. Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients. Int J Colorectal Dis. 2014;29(12):1527-1534. View Scientific Paper →
Sigalos JT, Pastuszak AW. The safety and efficacy of growth hormone secretagogues. Sex Med Rev. 2018;6(1):45-53. View Scientific Paper →
Sigalos JT, Pastuszak AW, Allison A, et al. Growth hormone secretagogue treatment in hypogonadal men raises serum insulin-like growth factor-1 levels. Am J Mens Health. 2017;11(6):1752-1757. View Scientific Paper →
Andersen NB, Malmlof K, Johansen PB, et al. The growth hormone releasing peptide ipamorelin reverses glucocorticoid-induced osteopenia in adult rats. Growth Horm IGF Res. 2001;11(4):266-272. View Scientific Paper →
Bowers CY. Unnatural growth hormone-releasing peptide begets natural ghrelin. JCEM. 2001;86(4):1464-1469. View Scientific Paper →
Veldhuis JD, Bowers CY. Integrating GHS into the ghrelin system. Int J Pept. 2010;2010:879503. View Scientific Paper →
Smith RG, Van der Ploeg LHT, Howard AD, et al. Peptidomimetic regulation of growth hormone secretion. Endocr Rev. 1997;18(5):621-645. View Scientific Paper →
Kojima M, Hosoda H, Date Y, et al. Ghrelin is a growth-hormone-releasing acylated peptide from stomach. Nature. 1999;402(6762):656-660. View Scientific Paper →