Nonapeptide-1 (Melanostatine-5) Cosmetic Ingredient Supplier — UPOR Biotech
Nonapeptide-1 (Melanostatine-5) — a selective α-MSH antagonist and MC1R blocker that inhibits melanin synthesis for skin brightening and even-tone correction. A nine-amino-acid peptide (Met-Pro-D-Phe-Arg-D-Trp-Phe-Lys-Pro-Val-NH₂) that works upstream at the melanocortin-1 receptor (MC1R) — reducing α-MSH-induced cAMP and melanosome dispersion without inhibiting tyrosinase. Cosmetic-grade bulk supplier for brightening serums and anti-pigmentation formulas from UPOR Biotech.
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Nonapeptide-1 (CAS 158563-45-2, C₆₁H₈₇N₁₅O₉S, MW 1206.5 g/mol) — trade name Melanostatine-5 — is a synthetic nine-amino-acid peptide with the sequence Met-Pro-D-Phe-Arg-D-Trp-Phe-Lys-Pro-Val-NH₂ (MPFRWFKPV-NH₂). It functions as a selective, competitive antagonist of the melanocortin-1 receptor (MC1R), binding with a Ki of ~40 nM to block α-melanocyte-stimulating hormone (α-MSH) signaling. By occupying MC1R, Nonapeptide-1 inhibits α-MSH-induced cAMP production (IC₅₀ ≈ 2.5 nM) and melanosome dispersion (IC₅₀ ≈ 11 nM) in melanocytes — the two upstream signals that drive melanin synthesis. Because it acts at the receptor rather than at tyrosinase, Nonapeptide-1 delivers targeted melanin reduction without the irritation associated with classic tyrosinase inhibitors such as hydroquinone or arbutin. This upstream control makes it a precise, gentle active for skin brightening, even-tone correction, and hyperpigmentation reduction.
As a cosmetic-grade active peptide supplier, UPOR Biotech provides high-purity Nonapeptide-1 (≥98.0% by HPLC) in white to off-white powder form for brightening serums, dark-spot correctors, and even-tone creams. Nonapeptide-1 is water-soluble and formulated in the aqueous phase at a remarkably low recommended usage rate of 1–10 ppm active, making it highly cost-efficient while remaining exceptionally gentle. It is compatible with pH 5.0–7.0 and pairs synergistically with niacinamide, vitamin C derivatives, and antioxidants for comprehensive brightening systems. The ingredient carries full cosmetic documentation — ISO 9001, cGMP, FDA facility registration, HALAL, KOSHER, and COSMOS compliance — supporting clean-label, globally compliant skincare. For brands, contract manufacturers, and private-label formulators, Nonapeptide-1 offers a differentiated anti-pigmentation mechanism backed by precise peptide chemistry and complete lot traceability.
Nonapeptide-1 (Melanostatine-5) vs Acetyl Hexapeptide-1 (Melitane) — α-MSH Antagonist (Brightening) vs α-MSH Agonist (Tanning)
The distinction between Nonapeptide-1 (Melanostatine-5) and Acetyl Hexapeptide-1 (Melitane) lies in how each peptide engages the melanocortin-1 receptor (MC1R). Nonapeptide-1 is a competitive MC1R antagonist — it blocks α-MSH signaling, inhibits melanin synthesis, and is used to brighten skin, even tone, and reduce dark spots. Melitane is an MC1R agonist — it mimics α-MSH, stimulates melanogenesis, and is positioned for tanning and skin pigmentation enhancement. In short, they are opposite mechanisms for opposite goals: antagonist for brightening/anti-pigmentation, agonist for tanning. For formulators developing brightening or spot-correcting products, Nonapeptide-1 is the correct MC1R-directed active — and its gentle, non-tyrosinase profile makes it safe for sensitive-skin brightening.
Technical Specifications
| Property | Specification |
|---|---|
| Product Name | Nonapeptide-1 (Melanostatine-5) — Cosmetic Grade |
| INCI Name | Nonapeptide-1 |
| Trade Name | Melanostatine-5 |
| CAS Number | 158563-45-2 |
| Molecular Formula | C₆₁H₈₇N₁₅O₉S |
| Molecular Weight | 1206.5 g/mol |
| Peptide Sequence | Met-Pro-D-Phe-Arg-D-Trp-Phe-Lys-Pro-Val-NH₂ |
| Peptide Class | 9-amino-acid α-MSH antagonist |
| Mechanism of Action | MC1R antagonist (Ki 40 nM) → inhibits melanin synthesis |
| Appearance | White to off-white powder |
| Purity (HPLC) | ≥98.0% |
| Assay Method | HPLC, area normalization |
| Peptide Content | ≥90.0% (by mass) |
| Water Content (Karl Fischer) | ≤5.0% |
| Heavy Metals (Total) | ≤10 ppm |
| Lead (Pb) | ≤1 ppm |
| Arsenic (As) | ≤1 ppm |
| Microbial Limits | TPC ≤100 CFU/g; negative pathogens |
| Solubility | Water-soluble; formulated in the aqueous phase |
| Recommended Usage Rate | 1 – 10 ppm active |
| pH | 5.0 – 7.0 |
| Grade | Cosmetic Grade |
| Certifications | ISO 9001, cGMP, FDA facility registration, HALAL, KOSHER, COSMOS |
| Packaging | 10 g / 100 g / 1 kg |
| Storage | 2–8°C or -20°C, protected from light and moisture |
| Shelf Life | 2 years |
| Disclaimer | For cosmetic formulation use |
Key Benefits — Nonapeptide-1
Selective MC1R Antagonism (Ki 40 nM)
Nonapeptide-1 competitively binds the melanocortin-1 receptor (MC1R) with a Ki of ~40 nM, selectively blocking α-MSH signaling. This receptor-level antagonism is highly targeted — interrupting the exact upstream signal that triggers melanin synthesis.
Ki 40 nMInhibits Melanin Synthesis & Melanosome Dispersion
Blocks α-MSH-induced cAMP (IC₅₀ ≈ 2.5 nM) and melanosome dispersion (IC₅₀ ≈ 11 nM) in melanocytes — the two signals required for melanin production. The result is measurable reduction in melanin synthesis and pigment transfer.
cAMP IC₅₀ 2.5 nMSkin Brightening & Even-Tone Action
Targets the melanogenesis pathway at its origin to deliver brighter, more even-toned skin — reducing dark spots, melasma, and post-inflammatory hyperpigmentation without aggressive exfoliation or irritation.
Brightening ActiveGentle Upstream Mechanism (Non-Tyrosinase)
Acts upstream of tyrosinase at MC1R, so it brightens without the irritation, redness, and barrier disruption commonly linked to direct tyrosinase inhibitors — ideal for sensitive-skin brightening.
Non-TyrosinaseApplications
Skin-Brightening & Whitening Serums
High-potency aqueous serums delivering 1–10 ppm Nonapeptide-1 as the core brightening active, targeting melanin reduction and luminosity.
Dark-Spot & Hyperpigmentation Correctors
Precision spot treatments for age spots, sun spots, and post-inflammatory hyperpigmentation via MC1R antagonism.
Even-Tone & Radiance Creams
Daily moisturizers and radiance creams formulated to unify skin tone and restore luminosity.
Melasma & Post-Inflammatory Pigmentation Care
Gentle care formulations for melasma-prone and post-blemish skin, reducing pigmentation without irritation.
Gentle Brightening for Sensitive Skin
Non-tyrosinase brightening systems suitable for sensitive and reactive skin types.
Clean-Label / COSMOS-Compliant Skincare
COSMOS-compliant, clean-label brightening products backed by HALAL/KOSHER and cGMP documentation.
Frequently Asked Questions
Nonapeptide-1 (Melanostatine-5) is a synthetic nine-amino-acid peptide (sequence Met-Pro-D-Phe-Arg-D-Trp-Phe-Lys-Pro-Val-NH₂, MW 1206.5 g/mol) that acts as a selective α-MSH antagonist. It competitively binds the melanocortin-1 receptor (MC1R, Ki ≈ 40 nM), blocking α-MSH signaling and inhibiting α-MSH-induced cAMP and melanosome dispersion. This reduces melanin synthesis at its source — delivering skin brightening, even tone, and hyperpigmentation reduction through a gentle, upstream mechanism.
They are functional opposites at the same receptor. Nonapeptide-1 is an MC1R antagonist — it blocks α-MSH signaling to inhibit melanin, producing skin brightening and anti-pigmentation effects. Acetyl Hexapeptide-1 (Melitane) is an MC1R agonist — it activates the receptor to stimulate melanogenesis, producing a tanning effect. Choose Nonapeptide-1 for brightening and spot reduction; choose Melitane for tanning enhancement.
Nonapeptide-1 is exceptionally potent — the recommended usage rate is 1–10 ppm (0.0001–0.001%) active in the finished cosmetic formula. It is water-soluble and added to the aqueous phase during formulation, ideally below 40°C to preserve peptide integrity. This ultra-low inclusion rate makes it highly cost-efficient for mass-market brightening lines while maintaining a gentle, irritation-free profile.
Incorporate Nonapeptide-1 into the aqueous phase at pH 5.0–7.0, adding it at cool-down (below 40°C) to protect the peptide. It is compatible with water-based serums, gels, and emulsions and pairs well with niacinamide, vitamin C derivatives, and antioxidants for synergistic brightening. Avoid extremes of pH, high heat, and strong chelators to preserve stability; store the raw material at 2–8°C or -20°C, protected from light and moisture.
Each cosmetic-grade shipment includes a full documentation package: COA (HPLC purity ≥98.0%, heavy metals ≤10 ppm, microbial limits), MSDS, HPLC chromatogram, mass spectrometry confirmation, COSMOS compliance statement, and HALAL, KOSHER, ISO 9001, cGMP, and FDA facility registration certificates. Complete lot traceability is provided from synthesis through final HPLC release — all documents in English.