Ipamorelin (10 mg)

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At a Glance

Ipamorelin is a synthetic pentapeptide GHS-R1a agonist that binds the ghrelin receptor on pituitary somatotrophs to trigger pulsatile GH release without raising cortisol or prolactin at research doses.[1] Sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH₂. CAS 170851-70-4. MW 711.85.[2]

• Reconstitute: Add 3.0 mL bacteriostatic water → 3.33 mg/mL concentration.
• Standard dose: 100–250 mcg subcutaneous, once daily, 30–60 minutes before bedtime on an empty stomach.
• Easy measuring: At 3.33 mg/mL on a U-100 syringe, 1 unit = 0.01 mL ≈ 33 mcg. A 100 mcg dose = 3 units / 0.03 mL; 200 mcg = 6 units / 0.06 mL; 250 mcg = 7.5 units / 0.075 mL.
• Storage: Lyophilised: refrigerate at 2–8 °C (freeze at −20 °C for long-term); reconstituted: refrigerate at 2–8 °C; use within 4 weeks.

Overview

• Goal: Stimulate pulsatile GH release from the pituitary with minimal cortisol or prolactin co-stimulation.[1]
• Schedule: One subcutaneous injection daily, on an empty stomach, 30–60 minutes before bedtime.
• Dose range: 100–250 mcg per injection, titrated over the cycle.
• Reconstitution: 3.0 mL BAC water per 10 mg vial → 3.33 mg/mL.
• Injection site: Abdomen, thigh, or upper arm; rotate daily.

What You'll Need

Plan based on a representative 8-week cycle dosed once daily and titrated (100 mcg weeks 1–2, 150 mcg weeks 3–4, 200 mcg weeks 5–8 — 56 injections, 9.1 mg total).

• Ipamorelin Vials (10 mg each): 9.1 mg needed ÷ 10 mg per vial → 1 vial covers the 8-week cycle with buffer.
• Insulin Syringes (U-100, 1 mL): 56 injections → 56 syringes.
• Bacteriostatic Water (10 mL bottles): 3.0 mL per vial → 1 × 10 mL bottle covers 3 vials.
• Alcohol Swabs: 2 per injection → 112 swabs per 8-week cycle.

How to Reconstitute

1. Allow the refrigerated lyophilised vial to reach room temperature (10–15 minutes).
2. Draw 3.0 mL bacteriostatic water with a sterile syringe.
3. Inject slowly down the inner vial wall; do not spray directly onto the powder.
4. Gently swirl or roll until dissolved. Do not shake. Solution should be clear and colourless.
5. Label with reconstitution date; refrigerate at 2–8 °C. Use within 4 weeks.

Dosing Schedule

Administer on an empty stomach 30–60 minutes before bedtime; eating within 1–2 hours before injection raises insulin, which suppresses GH secretion. A pre-sleep injection aligns with natural nocturnal GH pulsatility. At 3.33 mg/mL, one 10 mg vial provides 50 days at 200 mcg once daily, or 40 days at 250 mcg once daily.[1]

Protocol Details

• Weeks 1–2 (initiation): 100 mcg (3 units / 0.03 mL) once daily in the evening, for tolerance assessment.
• Weeks 3–4: 150 mcg (4.5 units / 0.045 mL) once daily.
• Weeks 5–8: 200 mcg (6 units / 0.06 mL) once daily.
• Weeks 9–12 (peak): 250 mcg (7.5 units / 0.075 mL) once daily.[1]
• Cycle length: 8–12 weeks on, with an optional extension to 16 weeks, followed by 2–4 weeks off. Rest periods allow GHS-R1a receptor sensitivity to recover.

Storage

• Lyophilised: Refrigerate at 2–8 °C (35–46 °F); freeze at −20 °C for storage beyond 3 months. Protect from light.
• Reconstituted: Refrigerate at 2–8 °C. Avoid freeze-thaw cycles. Use within 4 weeks.
• Appearance: Clear, colourless solution. Discard if cloudy, coloured, or particulate.

How Ipamorelin Works

Ipamorelin binds GHS-R1a (the ghrelin receptor) on pituitary somatotroph cells. Receptor activation couples to Gαq, triggering phospholipase C → IP₃ → intracellular calcium release, which drives GH secretion in discrete pulses that match the body's natural secretory pattern.[1]

The selectivity profile is ipamorelin's key pharmacological feature. GHRP-2 and GHRP-6 also bind GHS-R1a but engage receptors on the adrenal cortex and pituitary lactotrophs, raising cortisol and prolactin alongside GH. Ipamorelin's GHS-R1a selectivity means the ACTH/cortisol and PRL axes stay quiet at research doses.[1] The downstream effect is elevated IGF-1 and the anabolic, lipolytic, and recovery-associated signals driven by endogenous GH pulses.

Sequence: Aib-His-D-2-Nal-D-Phe-Lys-NH₂. Formula: C₃₈H₄₉N₉O₅. CAS 170851-70-4. MW 711.85.[2]

Good to Know

• Administer on an empty stomach; insulin from a recent meal blunts GH secretion.
• Pre-sleep timing takes advantage of the natural nocturnal GH surge; 30–60 minutes before bedtime is the standard once-daily window.
• A structured weekly titration (100 → 150 → 200 → 250 mcg) lets receptor response settle at each step before advancing.
• IGF-1 levels may rise over a cycle; long-term elevation warrants monitoring in individual research contexts.
• WADA status: GHS-R1a agonists are S2-class non-approved peptides. Athletes under anti-doping programmes must not use ipamorelin.
• For background on ipamorelin's mechanism, evidence, and research applications, see What Is Ipamorelin?.

Tips for Best Results

• Inject on an empty stomach, at least 1–2 hours after the last meal.
• Pre-sleep injection captures the nocturnal GH window; dose 30–60 minutes before bedtime.
• Pair with adequate protein (1.2–1.6 g/kg) and sleep (7–9 hours) to translate elevated GH/IGF-1 into tissue recovery.
• Avoid eating for at least 30–60 minutes post-injection to preserve the GH pulse.
• Track injection sites and rotate daily. Ipamorelin is typically well-tolerated subcutaneously, but rotation remains good practice.

Injection Tips

• Clean the vial stopper and injection site with separate alcohol swabs; allow both to air-dry fully before proceeding.
• Using a 29–31 gauge insulin syringe (5/16″ to 1/2″ needle), draw the calculated dose precisely.
• Pinch a fold of skin and insert the needle at 45° into subcutaneous fat (90° is acceptable with a short needle into a well-pinched fold).
• Inject slowly over 2–3 seconds; do not aspirate. Withdraw the needle, apply gentle pressure, and do not rub the site.
• Rotate injection sites (abdomen, thighs, upper arms) and dispose of each syringe in a sharps container immediately after use.[3]