Target Solvent
Bacteriostatic Water USP (0.9% Benzyl Alcohol)
Clear, colorless aqueous solution. Protect strictly from direct sunlight and repeated freezing.
Validated Laboratory Standard
Revision 1 · Lyophilized Solid Powder
Selective Pentapeptide Growth Hormone Secretagogue Receptor (GHS-R1a) Standard. Formulated for in-vitro research and laboratory analytical validation.
Selective Pentapeptide Growth Hormone Secretagogue Receptor (GHS-R1a) Standard. Formulated for in-vitro research and laboratory analytical validation.
What it is: Ipamorelin is a synthetic pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) that belongs to the Growth Hormone Secretagogue (GHS) family and acts as a selective ghrelin receptor agonist.
How it works: It selectively binds to the ghrelin/GHS-R1a receptor in the pituitary gland, triggering clean, natural pulses of growth hormone (GH) that closely mimic the body's natural youthful secretion patterns. Remarkably, unlike older GHRPs, Ipamorelin does not stimulate cortisol, prolactin, or ACTH, and causes minimal hunger spikes.
Why researchers study it: Studied for deep slow-wave sleep enhancement, lean muscle preservation, accelerated wound and bone healing, body fat reduction, skin collagen synthesis, and anti-aging without hormonal side effects.
Molecular Selectivity, Absence of Cortisol/Prolactin Elevation, and Pituitary Secretion Kinetics
Ipamorelin possesses the chemical sequence Aib-His-D-2-Nal-D-Phe-Lys-NH2, representing a meticulously engineered peptide backbone designed to resist rapid enzymatic hydrolysis by serum peptidases while maximizing steric complementarity to the binding pocket of the human GHS-R1a receptor.
The substitution of α-aminoisobutyric acid (Aib) at the N-terminus and D-stereoisomers at positions 3 and 4 confers robust proteolytic resistance against dipeptidyl peptidase IV (DPP-4) and aminopeptidases, granting Ipamorelin a plasma elimination half-life of approximately 2 hours in mammalian models—substantially longer than native ghrelin (half-life ~10-15 minutes).
With a monoisotopic molecular weight of 711.86 Da, Ipamorelin exists as an amphiphilic white lyophilized powder that readily dissolves in aqueous solvents, forming clear, non-aggregating solutions under neutral pH conditions.
Upon binding to the transmembrane G-protein coupled receptor GHS-R1a on somatotroph membranes of the anterior pituitary gland, Ipamorelin initiates a Gαq/11 signaling cascade. This triggers phospholipase C (PLC) activation, catalyzing the hydrolysis of phosphatidylinositol 4,5-bisphosphate (PIP2) into inositol 1,4,5-trisphosphate (IP3) and diacylglycerol (DAG).
IP3 diffuses to the endoplasmic reticulum, binding to IP3 receptors and prompting rapid mobilization of intracellular calcium stores. Concurrently, protein kinase C (PKC) activation induces closure of voltage-gated potassium channels, depolarizing the somatotroph membrane and opening L-type calcium channels. The resultant influx of extracellular calcium drives exocytic vesicle fusion, releasing pre-formed GH granules into circulation.
Crucially, radioligand binding studies demonstrate that Ipamorelin does not activate dopamine, opioid, or adrenergic receptors, explaining its complete lack of hyperprolactinemia or autonomic instability.
First-generation GH secretagogues (such as GHRP-6 and GHRP-2) are notorious for cross-reacting with hypothalamic corticotropin-releasing hormone (CRH) pathways, leading to dose-dependent elevations in ACTH, systemic cortisol, and prolactin. In longitudinal research models, prolonged hypercortisolemia induces catabolic muscle wasting, immune suppression, and insulin resistance.
Ipamorelin was structurally engineered to eliminate this cross-reactivity. In classic in-vivo porcine and rodent bioassays by Raun et al., escalating doses of Ipamorelin up to 50 times the ED50 elicited robust, dose-dependent growth hormone spikes while plasma cortisol and prolactin remained indistinguishable from baseline saline vehicle controls.
This unique endocrine fidelity establishes Ipamorelin as the benchmark reference standard for selective GH secretagogue research where unperturbed baseline adrenal and gonadal axes are required.
The downstream endocrine mediator of Ipamorelin-induced GH release is hepatic insulin-like growth factor 1 (IGF-1). Elevated circulating and paracrine IGF-1 stimulates the PI3K/Akt and MAPK/ERK pathways in peripheral tissues, stimulating skeletal muscle protein synthesis and osteoblast differentiation.
In longitudinal animal studies of osteopenia and bone demineralization, 12 weeks of daily Ipamorelin administration resulted in significant increases in cortical bone thickness, trabecular volumetric bone mineral density (vBMD), and mechanical loading strength compared to untreated controls.
Additionally, Ipamorelin enhances nitrogen balance in catabolic models, attenuating the muscle-wasting effects of prolonged glucocorticoid therapy or immobilized recovery states.
For analytical and in-vitro laboratory investigations, Ipamorelin lyophilized cake must be reconstituted with 0.9% USP grade bacteriostatic sodium chloride (0.9% benzyl alcohol preservative) or sterile water for injection (SWFI).
Recommended reconstitution volume is 2.0 mL of bacteriostatic diluent per 2mg or 5mg vial, gently directed down the inner glass wall of the borosilicate vial to minimize shear force denaturation. The vial should be swirled gently—never vortexed or shaken vigorously.
Reconstituted Ipamorelin must be shielded from ultraviolet photolysis and maintained in refrigerated storage at 2°C–8°C. Analytical stability testing confirms ≥98.5% peptide purity is preserved across 28 days of refrigerated storage.
Ipamorelin reference standard produced by Pepstack Labs conforms to strict analytical monograph specifications: purity ≥99.0% by reverse-phase high-performance liquid chromatography (RP-HPLC), mass identity verification by electrospray ionization mass spectrometry (ESI-MS, observed m/z 712.38 [M+H]+), and residual bacterial endotoxins <0.05 EU/mg by kinetic chromogenic LAL assay.
Storage Conditions: Store dry lyophilized powder at -20°C in an airtight container protected from desiccants and light for up to 24 months.
Regulatory & Safety Statement: This compound is synthesized and supplied strictly for in-vitro laboratory research, pharmacological profiling, and receptor binding assays. Not for human, veterinary, therapeutic, or cosmetic consumption.
Target Solvent
Bacteriostatic Water USP (0.9% Benzyl Alcohol)
Clear, colorless aqueous solution. Protect strictly from direct sunlight and repeated freezing.
Diluent Ratio
2 mL per 10 mg (5 mg/mL)
Direct 2.0 mL diluent slowly down the glass wall. Swirl in horizontal circular motions for 45 seconds until powder dissolves completely into an optical-grade transparent solution. Avoid shaking.
Lyophilized Storage
-20°C in dry desiccator (24 months)
Desiccated and protected from thermal spikes
Liquid Stability
2°C–8°C refrigerated; use within 28 days
Refrigerated and light-protected
Pharmacokinetics / Half-Life
~2 Hours (Selective somatotropic pulsatility without desensitization)
Typical protocol duration: 8 to 12 Weeks; Washout: 4 Weeks between cycles
| Standard Compound Mass | 10 mg active per vial |
| Recommended Diluent | Bacteriostatic Water USP (0.9% Benzyl Alcohol) |
| Diluent Volume Added | 2.0 mL |
| Resulting Concentration | 5.0 mg/mL |
| Syringe Volumetric Scale | U-100 Syringe (100 units = 1.0 mL | 1 unit = 50.0 mcg (0.01 mL)) |
| Handling Rule | Clear, colorless aqueous solution. Protect strictly from direct sunlight and repeated freezing. |
Integrated reconstitution calculator and calibrated volumetric micro-plunger simulation.
Benchmark protocols from peer-reviewed clinical trials & institutional investigational programs.
| Escalation Stage & Phase | Target Dose | U-100 Mark (10mg / 2.0mL) | Cadence | Syringe Sync |
|---|---|---|---|---|
| In-Vitro Assay Titration Schedule (Weeks 1–2) | 100 mcg | 2.0 Units(0.02 mL) | 1x Daily | |
| In-Vitro Assay Titration Schedule (Weeks 3–10) | 200 mcg | 4.0 Units(0.04 mL) | 1x Daily | |
| In-Vitro Assay Titration Schedule (Weeks 11–12) | 0 mcg | 0.0 Units(0.00 mL) | 1x Daily |
| Research Dose | Volume (mL) | U-100 Syringe Graduation Mark |
|---|---|---|
| 100 mcg (Micro Initiation) | 0.020 mL | 2 Units 2.0 units (0.02 mL) on U-100 syringe |
| 200 mcg (Standard Target) | 0.040 mL | 4 Units 4.0 units (0.04 mL) on U-100 syringe |
| 300 mcg (High Output Target) | 0.060 mL | 6 Units 6.0 units (0.06 mL) on U-100 syringe |
| Research Dose | Calibrated Volume | U-100 Syringe Units | Graduation Description |
|---|---|---|---|
| 100 mcg (Micro Initiation) | 0.02 mL (20 µL) | 2 Units | 2.0 units (0.02 mL) on U-100 syringe |
| 200 mcg (Standard Target) | 0.04 mL (40 µL) | 4 Units | 4.0 units (0.04 mL) on U-100 syringe |
| 300 mcg (High Output Target) | 0.06 mL (60 µL) | 6 Units | 6.0 units (0.06 mL) on U-100 syringe |
ISO 8537 Sterile Insulin Syringe Standard · Optical Meniscus Resolution & Volumetric Parallax Engineering
Detachable needles leave significant fluid trapped in the plastic hub collar. In peptide protocols, this causes substantial loss of active ingredient per administration.
| Barrel Capacity | Graduation Interval | Volume per Tick | Hub Dead-Space | Needle Spec | Suitability for 2 Units |
|---|---|---|---|---|---|
| 0.3 mL (30 Units)BEST FIT | 0.5 Unit | 5 µL (0.005 mL) | < 0.4 µL | 31G × 5/16" (8mm) Integrated Ultra-Fine | ✓ Accommodates 2 units |
| 0.5 mL (50 Units) | 1 Unit | 10 µL (0.010 mL) | < 0.8 µL | 30G–31G × 5/16" (8mm) Integrated | ✓ Accommodates 2 units |
| 1 mL (100 Units) | 2 Unit | 20 µL (0.020 mL) | < 2.1 µL | 29G–30G × 1/2" (12.7mm) Integrated | ✓ Accommodates 2 units |
Viewing the syringe from an angle introduces a 1.0–2.5 unit parallax error. Always raise the barrel to direct eye level against a high-contrast white background. Align the front edge of the top black plunger seal ring with the target line.
Standard 5/16" (8mm) laboratory dispensing needles are calibrated for direct 90° fluid transfer into target analytical matrix vials. If utilizing 1/2" (12.7mm) cannulas in deep laboratory vessels, introduce at a 45° angle to avoid contact with vessel sidewalls.
Stoichiometric supply planning, sequential reconstitution cadence, and itemized consumables BOM for Ipamorelin.
Do NOT reconstitute all 3 vials simultaneously. Reconstitute one vial at a time as the active protocol requires. Once reconstituted with Bacteriostatic Water USP, a vial maintains stability for 28 days at +2°C to +8°C. Remaining unopened vials should be preserved in solid lyophilized cake form at -20°C to prevent hydrolysis and oxidation.
| Week | Study / Assay Phase | Weekly Target Dose | Syringe Draw (U-100) | Active Vial # | Cumulative Active Mass |
|---|---|---|---|---|---|
| Week 1 | Phase 1: Baseline Secretagogue Calibration (Weeks 1–2) | 100 mcg(7x/wk) | 2 Units(0.02 mL) | Vial #1(9.3mg rem) | 0.7 mg / 26.6 mg |
| Week 2 | Phase 1: Baseline Secretagogue Calibration (Weeks 1–2) | 100 mcg(7x/wk) | 2 Units(0.02 mL) | Vial #1(8.6mg rem) | 1.4 mg / 26.6 mg |
| Week 3 | Phase 2: Target Somatotropic Pulsing (Weeks 3–10) | 200 mcg(7x/wk) | 4 Units(0.04 mL) | Vial #1(7.2mg rem) | 2.8 mg / 26.6 mg |
| Week 4 | Phase 2: Target Somatotropic Pulsing (Weeks 3–10) | 200 mcg(7x/wk) | 4 Units(0.04 mL) | Vial #1(5.8mg rem) | 4.2 mg / 26.6 mg |
| Week 5 | Phase 2: Target Somatotropic Pulsing (Weeks 3–10) | 200 mcg(7x/wk) | 4 Units(0.04 mL) | Vial #1(4.4mg rem) | 5.6 mg / 26.6 mg |
| Week 6 | Phase 2: Target Somatotropic Pulsing (Weeks 3–10) | 200 mcg(7x/wk) | 4 Units(0.04 mL) | Vial #1(3mg rem) | 7.0 mg / 26.6 mg |
| Week 7 | Phase 2: Target Somatotropic Pulsing (Weeks 3–10) | 200 mcg(7x/wk) | 4 Units(0.04 mL) | Vial #1(1.6mg rem) | 8.4 mg / 26.6 mg |
| Week 8 | Phase 2: Target Somatotropic Pulsing (Weeks 3–10) | 200 mcg(7x/wk) | 4 Units(0.04 mL) | Vial #1(0.2mg rem) | 9.8 mg / 26.6 mg |
| Week 9 | Phase 2: Target Somatotropic Pulsing (Weeks 3–10) | 200 mcg(7x/wk) | 4 Units(0.04 mL) | Vial #2(8.6mg rem) | 11.2 mg / 26.6 mg |
| Week 10 | Phase 2: Target Somatotropic Pulsing (Weeks 3–10) | 200 mcg(7x/wk) | 4 Units(0.04 mL) | Vial #2(7.2mg rem) | 12.6 mg / 26.6 mg |
| Week 11 | Phase 3: Pituitary Somatotrope Washout (Weeks 11–12) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #2(0.2mg rem) | 19.6 mg / 26.6 mg |
| Week 12 | Phase 3: Pituitary Somatotrope Washout (Weeks 11–12) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #3(3mg rem) | 26.6 mg / 26.6 mg |
Study duration: 8 to 12 Weeks · Washout: 4 Weeks between cycles
| Period / Phase | Target Amount | Frequency | Notes & Calibration |
|---|---|---|---|
| Weeks 1–2Starting Baseline | 100 mcg | 1x Daily (Pre-Bed SubQ, 2h post-prandial) | Phase 1: Baseline Secretagogue Calibration: GHS-R1a receptor binding calibration without cortisol, prolactin, or aldosterone elevation (2.0 units (0.02 mL) on U-100 syringe at 5.0 mg/mL concentration) |
| Weeks 3–10 | 200 mcg | 1x to 2x Daily (Morning Fasted / Pre-Bed) | Phase 2: Target Somatotropic Pulsing: Peak nocturnal growth hormone surge, slow-wave sleep enhancement, and lean tissue preservation (4.0 units (0.04 mL) on U-100 syringe (or 6.0 units for 300 mcg)) |
| Weeks 11–12 | Observation Period | Zero dosing | Phase 3: Pituitary Somatotrope Washout: Endogenous GHRH/somatostatin feedback equilibrium verification (4-week cessation window prevents pituitary receptor downregulation) |
4-phase stability timeline, RP-HPLC degradation benchmarks, and storage SOPs for Ipamorelin
Operating Window: +2°C to +8°C (36°F to 46°F)
Active working solution dissolved in Bacteriostatic Water USP (0.9% Benzyl Alcohol).
| Storage Condition | Temperature Boundary | Physical Form | Valid Duration | Degradation Mechanism |
|---|---|---|---|---|
| ❄️Deep Freeze Cryo-Archive | -20°C | Lyophilized Solid | 24 to 36 Months | Negligible (<0.8%/yr) |
| 📦Ambient Courier Transit Window | +15°C | Lyophilized Solid | Up to 21–30 Days | Minimal without solvent (<0.5%) |
| 💧Reconstituted Refrigerated Storage (2°C–8°C) | +2°C | Reconstituted Solution | 28 to 35 Days | Gradual deamidation >28 days |
| 🚫Critical Degradation Thresholds | >37°C | Degradation Hazard | Immediate Degradation Hazard | Rapid peptide cleavage & aggregation |
Direct 2.0 mL diluent slowly down the glass wall. Swirl in horizontal circular motions for 45 seconds until powder dissolves completely into an optical-grade transparent solution. Avoid shaking.
Ipamorelin displays an estimated half-life of ~2 Hours (Selective somatotropic pulsatility without desensitization). Typical study protocols run for 8 to 12 Weeks followed by a washout period of 4 Weeks between cycles.
High-purity lyophilized laboratory reference formulation with certified Certificate of Analysis (COA).
Standard Lyophilized Monograph
Selective Pentapeptide Growth Hormone Secretagogue Receptor (GHS-R1a) Standard. Formulated for in-vitro research and laboratory analytical validation.
Store desiccated at -20°C upon receipt. Reconstitute strictly in a certified laminar airflow hood utilizing sterile disposable instruments. Avoid direct exposure to UV or fluorescent radiation.
| Net Active Mass | Target Solvent | Diluent Volume | Resulting Concentration | Syringe Graduation Scale |
|---|---|---|---|---|
| 10 mg Lyophilized Cake | Bacteriostatic Water USP (0.9% Benzyl Alcohol) | 2.0 mL | 5.00 mg/mL | 1 Unit = 50.0 mcg (0.01 mL) |
Swab vial septum with sterile 70% IPA pad. Inspect cake for vacuum seal integrity.
Introduce 2.0 mL solvent slowly down inner glass wall. Never spray directly on cake.
Swirl gently in horizontal circles until fully dissolved. Never shake or invert aggressively.
Rest at +2°C to +8°C for 10 minutes until solution is crystal clear before drawing.
| Phase | Target Active Dose | U-100 Syringe Graduation | Cadence & Pharmacological Purpose |
|---|---|---|---|
| Days 1–7 (Priming) | 100 mcg | 2.0 Units (0.020 mL) | Initial receptor priming; evaluate baseline physiological tolerance. |
| Weeks 2–4 (Saturation) | 150 mcg | 3.0 Units (0.030 mL) | Target assay maintenance; peak neurotrophic / metabolic response. |
| Weeks 5–6 (Taper & Washout) | 100 mcg | 2.0 Units (0.020 mL) | Receptor consolidation prior to mandatory 4-week washout cycle. |
RP-HPLC / LC-MS In-Vitro Assay
Purity Spec: ≥ 98.0% Area
Research Use Only (RUO)
NOT EVALUATED OR APPROVED BY FDA