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.
Melanotan I Dosage Chart, Schedule & Reconstitution Protocol
Quickstart Highlights
Melanotan I (afamelanotide, Scenesse) is a synthetic 13-amino-acid α-MSH analogue and MC1R agonist that drives eumelanin synthesis and photoprotection without UV light (PMID 16763547, PMID 28063031). Its only approved use is a 16 mg controlled-release subcutaneous implant inserted every 2 months for erythropoietic protoporphyria, FDA-approved 2019 and EMA-approved 2014 (PMID 26132941). In grey-market cosmetic tanning, a reconstituted liquid is injected at about 250 mcg/day for a 10-14 day loading phase, then 250-500 mcg every 3-4 days; this use is unapproved and unvalidated. The peptide's intrinsic plasma half-life is very short (~30 minutes), but the implant releases over ~2 days with an apparent half-life near 15 hours, and the visible tan lasts for weeks. The subcutaneous liquid figures here are an educational measurement reference, not medical advice.
Reconstitute: Add 2 mL bacteriostatic water → 5 mg/mL concentration.
Typical dose: 250 mcg/day SC (loading), then 250-500 mcg every 3-4 days
Easy measuring: At 5 mg/mL, 1 unit = 0.01 mL = 0.0500 mg (50 mcg) on a U-100 insulin syringe.
Storage: Lyophilized powder stored frozen at −20 °C and protected from light; once reconstituted, refrigerate at 2-8 °C, shield from light, and use within roughly 4 weeks. The approved Scenesse implant is stored refrigerated at 2-8 °C and handled only by the implanting clinic.
Half-life: Intrinsic peptide ~0.1-0.5 h (~30 min); from the controlled-release implant Tmax ~36 h, apparent half-life ~15 h, undetectable by ~day 10. Tan persists for weeks.
Route: Parenteral only — approved as a 16 mg subcutaneous implant; not orally bioavailable. The daily SC liquid figures here are an educational reconstitution reference.
Status: FDA- and EMA-approved (as Scenesse) only for erythropoietic protoporphyria; NOT approved for cosmetic tanning. Injectable liquid is unlicensed/research use only.
About Melanotan I
Melanotan I (afamelanotide) is a synthetic α-melanocyte-stimulating hormone (α-MSH) analogue that acts as a selective melanocortin-1 receptor (MC1R) agonist, switching melanocytes toward production of eumelanin, the dark, UV-absorbing pigment, without requiring sun exposure [2][3]. It is important to be honest about route: the clinically approved product is NOT a daily injection. It is a 16 mg controlled-release implant (Scenesse) that a physician inserts subcutaneously above the iliac crest every two months for erythropoietic protoporphyria [1][4]. The daily subcutaneous liquid figures below model the separate research/grey-market \"tanning\" protocol and are an educational reconstitution reference only, not the approved regimen.\n\nThis guide models a 10 mg vial reconstituted with 2 mL of bacteriostatic water (5 mg/mL, i.e. 50 mcg per insulin-syringe unit) so that research doses land cleanly on a U-100 syringe: 125 mcg ≈ 2.5 units, 250 mcg ≈ 5 units, and 500 mcg ≈ 10 units. The most commonly described approach is a 10-14 day loading phase at about 250 mcg once daily (often started lower to gauge nausea and flushing), followed by 250-500 mcg every 3-4 days for maintenance.\n\nFrequency: Inject once daily during the loading phase, then about 2-3 times per week for maintenance. Melanotan I in this injectable form is not approved for cosmetic tanning by the FDA, EMA, MHRA or TGA; this page is educational only and not medical advice [6][8].
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 2 mL of bacteriostatic water into a sterile syringe.
Inject the water slowly down the inner wall of the 10 mg Melanotan I vial; never aim the stream directly at the powder and do not shake.
Gently swirl or roll the vial until the solution is completely clear; this yields a 5 mg/mL concentration (50 mcg per U-100 insulin-syringe unit).
Store the reconstituted vial refrigerated at 2-8 °C, protected from light, and draw the prescribed units per dose (125 mcg ≈ 2.5 units, 250 mcg ≈ 5 units, 500 mcg ≈ 10 units).
Educational note: the regulator-approved form is a clinician-inserted 16 mg implant, not a daily injection — these subcutaneous liquid figures are a measurement reference only; for educational SC modeling, insert into abdominal subcutaneous tissue, inject slowly, and discard the dose if the solution is cloudy or discolored.
Interactive Melanotan I Syringe Calculator
Currently visualizing the 10 mg vial reconstituted with 2 mL bacteriostatic water. Adjust the target dose to dynamically render syringe units.
Reconstitution Calculation: 10mg dry powder in 2mL water yields 5.00 mg/mL. To evaluate a 250mcg dose, pull to 5.0 units (5 syringe ticks).
U-100 Syringe Representation
Educational reference visual. Assumes standard U-100 insulin syringe where 1.0 mL volume = 100 units.
Titration & Dose Escalation Schedules
| Phase | Dose per injection | Units (per injection) |
|---|---|---|
| Days 1-3 — titration start (assess nausea/flushing) | 125 mcg | 3 units (0.03 mL) |
| Days 4-14 — loading phase, once daily | 250 mcg | 5 units (0.05 mL) |
| Maintenance — 250 mcg every 3-4 days | 250 mcg | 5 units (0.05 mL) |
| Maintenance (higher) — 500 mcg every 3-4 days | 500 mcg | 10 units (0.10 mL) |
Administration guidelines: Refer to guidelines | 2 mL Reconstitution
Research Supplies Quantity Planner
Scientific mathematical planning of syringes, bacteriostatic water and dry vials needed for extended research blocks using the 10 mg vial.
Peptide Vials (Melanotan I, 10 mg each):
- check8-week course (loading + maintenance) ≈ 1-2 vials
- check12-week course ≈ 2 vials
- check16-week course ≈ 2-3 vials (higher 500 mcg maintenance pushes toward 3)
Insulin Syringes (U-100):
- checkOne syringe per injection (daily during loading, ~2-3 weekly maintenance)
- check8 weeks ≈ 28-35 syringes; 12 weeks ≈ 40-50 syringes
- check16 weeks ≈ 50-65 syringes; keep spares for re-draws
Bacteriostatic Water (30 mL bottles): Use 2 mL per 10 mg vial for reconstitution.
- check8 weeks (1-2 vials) ≈ 2-4 mL
- check12 weeks (2 vials) ≈ 4 mL
- check16 weeks (2-3 vials) ≈ 4-6 mL — a single 30 mL bottle covers a full course
Alcohol Swabs:
- check1-2 swabs per dose (vial septum + injection site)
- check8 weeks ≈ 50-70 swabs; 12 weeks ≈ 80-100 swabs
- check16 weeks ≈ 100-130 swabs; keep extras for re-swabbing the multi-use vial
Mechanism of Action (MOA)
Melanotan I (afamelanotide) is a linear tridecapeptide (13 amino acids) that copies the core sequence of human α-melanocyte-stimulating hormone (α-MSH) with two deliberate engineering changes: methionine at position 4 is replaced by norleucine (Nle) and L-phenylalanine at position 7 by D-phenylalanine (D-Phe), giving the molecule [Nle4,D-Phe7]-α-MSH [2][3]. These substitutions block the proteolytic cleavage and oxidation that rapidly destroy native α-MSH, so the analogue is markedly more stable and, in bioassays, roughly 100-1000 times more potent than the natural hormone [2].\n\nIts target is the melanocortin-1 receptor (MC1R), a Gs-protein-coupled receptor on epidermal melanocytes. Agonism activates adenylate cyclase, raising intracellular cyclic AMP, which upregulates the transcription factor MITF and the rate-limiting enzyme tyrosinase. The net effect is a shift of melanogenesis away from reddish, weakly protective pheomelanin toward dark, UV-absorbing eumelanin, producing tanning and photoprotection without UV exposure [2][3]. MC1R signaling additionally enhances antioxidant defenses, DNA-repair capacity (reducing thymine-dimer and sunburn-cell formation after UV), and dampens inflammation [2][3]. Unlike Melanotan II, a cyclic peptide that broadly activates MC1R, MC3R, MC4R and MC5R (hence its strong libido, appetite and cardiovascular effects), Melanotan I is comparatively more MC1R-directed, which is why its principal cosmetic effect is pigmentation.\n\nPharmacokinetics depend heavily on the delivery format. The intrinsic peptide is short-lived: after intravenous or bolus exposure, plasma elimination half-life is only about 0.1-0.5 hours (roughly 30 minutes), and the peptide is broken down intracellularly by proteases into its constituent amino acids [3][6]. The approved Scenesse product circumvents this with a bioresorbable controlled-release implant: drug is released over about two days, reaches median peak plasma concentration (Tmax) near 36 hours, shows an apparent half-life of approximately 15 hours, and becomes undetectable in plasma by roughly day 10 [3][4]. A reconstituted research liquid injected subcutaneously therefore clears from blood within hours, but the visible pigmentary effect persists for days to weeks because newly synthesized eumelanin is durable. Route is exclusively parenteral; the peptide is not orally bioavailable, so there is no oral version, and the subcutaneous liquid figures on this page are an educational measurement convention rather than the clinically validated implant regimen.\n\nClinically, MC1R-driven pigmentation translated into longer pain-free sunlight tolerance and improved quality of life in erythropoietic protoporphyria, the indication for which afamelanotide is approved [1][4][5]. In healthy volunteers the same mechanism increased melanin density and reduced UV-induced DNA damage [2]. For cosmetic tanning, however, the injectable liquid is unlicensed, its purity is unverified, and its long-term safety is undocumented [6][8].
Clinical Trial Efficacy Highlights
- starLangendonk, Balwani and colleagues (NEJM, 2015) pooled two multicenter, randomized, double-blind, placebo-controlled trials (74 EU and 94 US patients) of the 16 mg subcutaneous implant every 60 days in erythropoietic protoporphyria; afamelanotide increased pain-free sun-exposure time and improved quality of life with an acceptable adverse-event profile, the data that supported regulatory approval [1].
- starBarnetson and colleagues (J Invest Dermatol, 2006) gave subcutaneous [Nle4,D-Phe7]-α-MSH (Melanotan I) at 0.16 mg/kg in three 10-day cycles to 65 fair-skinned volunteers; melanin density rose significantly (about 41% in the lowest-MED subjects), epidermal sunburn cells fell by more than 50%, and basal-layer thymine-dimer formation was reduced by roughly 59% versus placebo, demonstrating UV-independent photoprotection [2].
- starMinder and Barman-Aksözen (Clin Pharmacokinet, 2017) reviewed afamelanotide pharmacokinetics and pharmacodynamics, documenting MC1R-mediated increases in melanin synthesis, antioxidant activity, DNA repair and anti-inflammatory signaling, and detailing the implant release profile (Tmax ~36 h, apparent half-life ~15 h, undetectable by ~day 10) versus the very short intrinsic plasma half-life of the peptide [3].
- starBiolcati and colleagues (Br J Dermatol, 2015) reported a long-term observational study of afamelanotide in 115 EPP patients followed for up to several years; repeated implants sustained improvements in sun tolerance and quality of life without new long-term safety signals, supporting durability of the approved regimen [7].
- starThe FDA prescribing information for Scenesse (2019, NDA 210797) specifies the approved dose as a single 16 mg implant inserted subcutaneously above the anterior iliac crest every 2 months and confirms the indication is limited to increasing pain-free light exposure in adults with a history of phototoxic reactions from EPP [4].
- starThe European Medicines Agency authorized Scenesse for EPP in December 2014 (five years before the US), establishing afamelanotide as the first approved systemic photoprotective agent and providing the European efficacy and safety dataset [5].
- starA systematic review by Brennan and colleagues (Performance Enhancement & Health, 2014) of melanotan clinical trials and case reports found that controlled-trial side effects were largely minor (nausea, naevi darkening, yawning), but flagged systemic toxidrome and melanoma case reports and emphasized that long-term outcomes from unregulated injectable use remain undocumented [8].
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.
- warningNausea is the most consistent effect, reported in roughly 19% of implant recipients (versus ~14% on placebo) and frequently in injectable-liquid users; flushing, fatigue, dizziness, headache and somnolence are also common [1][4].
- warningImplant- or injection-site reactions (pain, swelling, discoloration) occurred in about 21% of treated patients versus ~10% with placebo in the approval trials [1][4].
- warningGeneralized skin darkening is expected and intended, but moles and other pigmented lesions also darken; this can obscure early melanoma and is why a full-body skin examination twice yearly is advised for treated patients [4].
- warningCase reports describe new or rapidly changing naevi and melanoma diagnoses associated with melanotan use; a causal link is unproven, but the signal is taken seriously and is a key reason cosmetic use is discouraged [6][8].
- warningBecause the injectable cosmetic product is unlicensed and grey-market, vials may be contaminated, mislabeled or wrongly dosed; injection of non-sterile or impure material adds infection and unknown-impurity risks beyond the peptide itself [6][8].
- warningCompared with Melanotan II, Melanotan I is more MC1R-selective and tends to produce fewer libido, spontaneous-erection and appetite effects, but nausea and flushing still occur via melanocortin signaling [3][8].
- warningAfamelanotide has not been linked to clinically significant liver enzyme elevations (LiverTox likelihood score E), but long-term systemic safety of repeated unregulated dosing is not established [6].
- warningRegulatory/research status: the injectable liquid is NOT approved for cosmetic tanning by the FDA, EMA, MHRA or TGA; only the 16 mg implant is approved, and only for EPP. This page is educational only and not medical advice [4][5][6].
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 Melanotan I dosage?expand_more
Two very different regimens exist. The only approved Melanotan I dosage is the Scenesse implant: a single 16 mg controlled-release implant inserted subcutaneously by a clinician every 2 months for erythropoietic protoporphyria. In research and grey-market cosmetic-tanning use, a reconstituted injectable liquid is dosed at roughly 250 mcg subcutaneously once daily for a 10-14 day loading phase (often started lower at ~125 mcg to gauge nausea and flushing), then 250-500 mcg every 3-4 days for maintenance. The injectable cosmetic protocol is unapproved and unvalidated; the figures here are educational only, not medical advice.
Is Melanotan I FDA approved?expand_more
Partly. The FDA approved Melanotan I as Scenesse (afamelanotide) in October 2019, but only as a 16 mg subcutaneous implant and only to increase pain-free light exposure in adults with erythropoietic protoporphyria (EPP). It is NOT approved for cosmetic tanning in any form. The injectable liquid sold online for tanning is an unlicensed research material; the FDA, MHRA and TGA have all warned against buying or using it. The EMA approved Scenesse for EPP earlier, in December 2014.
What is the half-life of Melanotan I?expand_more
It depends on the format. The peptide itself is short-lived: after bolus or intravenous exposure the plasma elimination half-life is only about 0.1-0.5 hours (roughly 30 minutes), and it is broken down by proteases into amino acids. The approved implant changes this by releasing drug slowly over about two days, giving a peak plasma level near 36 hours, an apparent half-life of approximately 15 hours, and undetectable plasma levels by about day 10. A reconstituted liquid injection clears from blood within hours, but the resulting tan persists for days to weeks because the new eumelanin is durable.
How is Melanotan I reconstituted and administered for research?expand_more
For the educational subcutaneous model on this site, a 10 mg vial is mixed with 2 mL of bacteriostatic water to give 5 mg/mL (50 mcg per U-100 insulin-syringe unit). Draw the water slowly down the vial wall, swirl gently until clear, and refrigerate protected from light. At that concentration, 125 mcg is about 2.5 units, 250 mcg is about 5 units, and 500 mcg is about 10 units. Remember the clinically approved product is a clinician-inserted implant, not a self-injected liquid; this reconstitution is a measurement reference only.
How is Melanotan I different from Melanotan II?expand_more
Melanotan I (afamelanotide) is a linear 13-amino-acid α-MSH analogue that is comparatively selective for the melanocortin-1 receptor (MC1R), the receptor that drives skin pigmentation. Melanotan II is a smaller cyclic peptide that broadly activates MC1R, MC3R, MC4R and MC5R, which is why it produces strong libido, spontaneous-erection and appetite effects in addition to tanning. Melanotan I is the only one of the two that reached regulatory approval (as Scenesse for EPP); Melanotan II has never been approved and is sold only as an unregulated research chemical.
Related Guides & Tools
Step-by-step references for reconstituting, measuring, and storing Melanotan I, plus the universal dosing calculator.
Academic References & Study Citations
Langendonk JG, Balwani M, Anderson KE, et al. Afamelanotide for Erythropoietic Protoporphyria. N Engl J Med. 2015;373(1):48-59. View Scientific Paper →
Barnetson RS, Ooi TK, Zhuang L, et al. [Nle4-D-Phe7]-alpha-melanocyte-stimulating hormone significantly increased pigmentation and decreased UV damage in fair-skinned Caucasian volunteers. J Invest Dermatol. 2006;126(8):1869-1878. View Scientific Paper →
Minder EI, Barman-Aksözen J. Pharmacokinetics and Pharmacodynamics of Afamelanotide and its Clinical Use in Treating Dermatologic Disorders. Clin Pharmacokinet. 2017;56(8):815-823. View Scientific Paper →
SCENESSE (afamelanotide) implant, for subcutaneous use — FDA Prescribing Information (NDA 210797), 2019. View Scientific Paper →
European Medicines Agency. Scenesse (afamelanotide) — EPAR (authorized for erythropoietic protoporphyria, December 2014). View Scientific Paper →
Afamelanotide. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. Bethesda (MD): NIH/NIDDK. View Scientific Paper →
Biolcati G, Marchesini E, Sorge F, et al. Long-term observational study of afamelanotide in 115 patients with erythropoietic protoporphyria. Br J Dermatol. 2015;172(6):1601-1612. View Scientific Paper →
Brennan R, Wells JSG, Van Hout MC. An unhealthy glow? A review of melanotan use and associated clinical outcomes. Performance Enhancement & Health. 2014;3(2):78-92. View Scientific Paper →