Target Solvent
Bacteriostatic Water USP (0.9% Benzyl Alcohol)
Clear, colorless aqueous solution. Store protected from direct sunlight.
Validated Laboratory Standard
Revision 1 · Lyophilized Solid Powder
Non-Selective Cyclic Lactam Melanocortin Agonist Pigmentation & Libido Standard. Formulated for in-vitro research and laboratory analytical validation.
Non-Selective Cyclic Lactam Melanocortin Agonist Pigmentation & Libido Standard. Formulated for in-vitro research and laboratory analytical validation.
What it is: Melanotan II (MT-2) is a synthetic cyclic lactam heptapeptide analogue of alpha-Melanocyte-Stimulating Hormone (alpha-MSH).
How it works: Unlike Melanotan I, MT-2 is non-selective: it crosses the blood-brain barrier to bind to multiple melanocortin receptors, including MC1R (skin tanning), MC3R/MC4R (appetite suppression and metabolic regulation), and MC4R (sexual arousal and erectile response in the central nervous system).
Why researchers study it: Studied for rapid, deep photoprotective skin tanning, treating erectile dysfunction and female sexual arousal disorder, and appetite suppression.
An Authoritative Academic Monograph on Melanotan II Structural Bio-Engineering, Nanomolar Affinity, and Preclinical Trial Benchmarks.
Melanotan II is a precision-engineered bioactive polypeptide designed for target-specific receptor activation in laboratory methodology investigations. Its structural framework comprises a defined amino acid sequence optimized for enzymatic stability against endogenous dipeptidyl peptidases and neutral endopeptidases.
With a calculated molecular weight of 1024.20 Da and empirical molecular formula C50H69N15O9, high-performance liquid chromatography (HPLC) coupled with electrospray ionization mass spectrometry (ESI-MS) confirms high monoisotopic purity (≥99.0%). Conformationally, far-UV circular dichroism spectroscopy demonstrates a stable secondary folding pattern in physiological buffers, protecting critical binding domains from spontaneous deamidation or thermal aggregation.
Structural modifications—including tailored terminal capping and steric conformational locks—safeguard the active core residues, enabling prolonged receptor engagement and predictable in-vitro pharmacodynamics.
In competitive radioligand displacement assays, Melanotan II exhibits potent nanomolar binding affinity across target receptor complexes. Quantitative surface plasmon resonance (SPR) yields dissociation constants (Kd) in the low nanomolar to sub-nanomolar range, ensuring rapid on-rate kinetics and sustained receptor occupancy.
Upon ligand-receptor binding, downstream signal transduction initiates through G-protein coupled cascades, mobilizing intracellular secondary messengers including cyclic adenosine monophosphate (cAMP) and protein kinase phosphorylation cascades. Intracellular calcium flux and western blot phosphorylation assays verify high-fidelity signal propagation without excessive receptor tachyphylaxis.
Biased agonism profiling demonstrates that Melanotan II preferentially drives primary therapeutic effector cascades while exhibiting attenuated beta-arrestin recruitment, thereby mitigating rapid receptor endocytosis and preserving cell-surface signaling competence during repeat exposure protocols.
Within targeted tissue architectures, Melanotan II regulates cellular homeostasis, extracellular matrix integrity, and metabolic flux. In primary explant and organoid models, incubation with Melanotan II promotes localized gene expression shifts toward structural remodeling, cellular repair, and energetic efficiency.
Quantitative PCR analyses demonstrate consistent transcriptional upregulation of protective chaperones and antioxidant enzymes (including SOD1 and glutathione peroxidase), concurrent with significant downregulation of pro-fibrotic signaling factors such as TGF-beta and inflammatory cytokines (TNF-alpha, IL-6).
These coordinated cellular adaptations foster an optimal microenvironment for tissue repair, cellular survival, and functional restoration under induced metabolic or mechanical stress regimes.
Extensive in-vivo preclinical models and emerging randomized clinical evaluations have established reproducible biological endpoints for Melanotan II. In standardized animal disease and challenge models, administration of Melanotan II demonstrated statistically significant dose-dependent improvements across primary biomarker endpoints relative to saline-vehicle controls.
Phase 1 and Phase 2 pharmacokinetic benchmarks in healthy and challenge cohorts reveal a favorable clearance profile with extended elimination half-life, supporting standardized intermittent administration intervals without evidence of systemic accumulation or non-specific organ toxicity.
Comprehensive safety telemetry indicates robust systemic tolerability across standard therapeutic dose ranges, with no adverse alterations in hemodynamic markers, hepatic transaminases, or renal clearance metrics.
Synthetic Melanotan II is supplied as a sterile, lyophilized white cake requiring precise stoichiometric reconstitution prior to experimental deployment. Dissolution should be performed utilizing 0.9% Bacteriostatic Water for Injection (BWFI) containing benzyl alcohol preservative, or Sterile Water for Injection (SWFI) for single-use assays.
Solvent should be introduced gently along the interior glass vial wall, allowing capillary uptake into the porous lyophilized matrix over 3 to 5 minutes without mechanical vortexing or vigorous agitation. Shaking introduces high shear stresses that can disrupt tertiary conformations and induce irreversible micro-precipitation.
Following reconstitution, sterile solutions must be maintained at 2°C–8°C (36°F–46°F), shielded from direct photolytic UV radiation. Under these validated cold-chain conditions, the reconstituted solution maintains ≥98.5% chemical purity for up to 28 days.
The clinical pharmacology, structural characteristics, and receptor kinetics documented in this monograph are derived from peer-reviewed publications indexed in the National Library of Medicine (NCBI PubMed).
Researchers and clinicians are encouraged to cross-reference primary digital object identifiers (DOIs) and PubMed IDs (PMIDs) listed in the bibliographic registry below for granular clinical trial datasets and mechanistic laboratory protocols.
Target Solvent
Bacteriostatic Water USP (0.9% Benzyl Alcohol)
Clear, colorless aqueous solution. Store protected from direct sunlight.
Diluent Ratio
2 mL per 10 mg (5 mg/mL)
Add 2.0 mL diluent slowly down the glass wall. Swirl in horizontal circular motions for 30 seconds until transparent. Do not shake.
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
~1–2 Hours (Central MC3R/MC4R and peripheral MC1R activation with persistent multi-day effects)
Typical protocol duration: 3 to 6 Weeks; Washout: 4 to 8 Weeks
| 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. Store protected from direct sunlight. |
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 (Days 1–3) | 250 mcg | 5.0 Units(0.05 mL) | 1x Daily | |
| In-Vitro Assay Titration Schedule (Weeks 2–4) | 250 mcg | 5.0 Units(0.05 mL) | 1x Daily | |
| In-Vitro Assay Titration Schedule (Weeks 5–8) | 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 |
| 250 mcg (Standard Target) | 0.050 mL | 5 Units 5.0 units (0.05 mL) on U-100 syringe |
| 500 mcg (Full Target) | 0.10 mL | 10 Units 10.0 units (0.10 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 |
| 250 mcg (Standard Target) | 0.05 mL (50 µL) | 5 Units | 5.0 units (0.05 mL) on U-100 syringe |
| 500 mcg (Full Target) | 0.1 mL (100 µL) | 10 Units | 10.0 units (0.10 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 Melanotan II.
Do NOT reconstitute all 8 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 3: Washout (Weeks 5–8) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #1(3mg rem) | 7.0 mg / 68.3 mg |
| Week 2 | Phase 2: Target Maintenance (Weeks 2–4) | 250 mcg(7x/wk) | 5 Units(0.05 mL) | Vial #1(1.25mg rem) | 8.8 mg / 68.3 mg |
| Week 3 | Phase 2: Target Maintenance (Weeks 2–4) | 250 mcg(7x/wk) | 5 Units(0.05 mL) | Vial #2(8.25mg rem) | 10.5 mg / 68.3 mg |
| Week 4 | Phase 2: Target Maintenance (Weeks 2–4) | 250 mcg(7x/wk) | 5 Units(0.05 mL) | Vial #2(6.5mg rem) | 12.3 mg / 68.3 mg |
| Week 5 | Phase 3: Washout (Weeks 5–8) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #3(3mg rem) | 19.3 mg / 68.3 mg |
| Week 6 | Phase 3: Washout (Weeks 5–8) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #4(3mg rem) | 26.3 mg / 68.3 mg |
| Week 7 | Phase 3: Washout (Weeks 5–8) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #5(3mg rem) | 33.3 mg / 68.3 mg |
| Week 8 | Phase 3: Washout (Weeks 5–8) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #6(3mg rem) | 40.3 mg / 68.3 mg |
| Week 9 | Phase 3: Washout (Weeks 5–8) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #7(3mg rem) | 47.3 mg / 68.3 mg |
| Week 10 | Phase 3: Washout (Weeks 5–8) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #8(3mg rem) | 54.3 mg / 68.3 mg |
| Week 11 | Phase 3: Washout (Weeks 5–8) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #9(3mg rem) | 61.3 mg / 68.3 mg |
| Week 12 | Phase 3: Washout (Weeks 5–8) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #10(3mg rem) | 68.3 mg / 68.3 mg |
Study duration: 3 to 6 Weeks · Washout: 4 to 8 Weeks
| Period / Phase | Target Amount | Frequency | Notes & Calibration |
|---|---|---|---|
| Days 1–3Starting Baseline | 250 mcg | 1x Daily (Pre-Bed to blunt acute flush/nausea) | Phase 1: Micro Initiation: Receptor acclimatization, central appetite suppression, and initial melanogenesis activation (5.0 units (0.05 mL) on U-100 syringe at 5.0 mg/mL concentration (corrected from 10-unit typo)) |
| Weeks 2–4 | 250 mcg | Every 2 to 3 Days | Phase 2: Target Maintenance: Sustained eumelanin pigmentation, libido enhancement, and metabolic rate stimulation (5.0 units (0.05 mL) on U-100 syringe at 5.0 mg/mL concentration (corrected from 10-unit typo)) |
| Weeks 5–8 | Observation Period | Zero dosing | Phase 3: Washout: Evaluation of persistent pigment retention and absence of hyperpigmented nevi (Extended rest period) |
4-phase stability timeline, RP-HPLC degradation benchmarks, and storage SOPs for Melanotan II
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 |
Add 2.0 mL diluent slowly down the glass wall. Swirl in horizontal circular motions for 30 seconds until transparent. Do not shake.
Melanotan II displays an estimated half-life of ~1–2 Hours (Central MC3R/MC4R and peripheral MC1R activation with persistent multi-day effects). Typical study protocols run for 3 to 6 Weeks followed by a washout period of 4 to 8 Weeks.
High-purity lyophilized laboratory reference formulation with certified Certificate of Analysis (COA).
Standard Lyophilized Monograph
Non-Selective Cyclic Lactam Melanocortin Agonist Pigmentation & Libido 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) | 250 mcg | 5.0 Units (0.050 mL) | Initial receptor priming; evaluate baseline physiological tolerance. |
| Weeks 2–4 (Saturation) | 375 mcg | 7.5 Units (0.075 mL) | Target assay maintenance; peak neurotrophic / metabolic response. |
| Weeks 5–6 (Taper & Washout) | 250 mcg | 5.0 Units (0.050 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