Melanotan-1 Spray is a product form of synthetic polypeptide Melanotan-1 made into nasal spray or oral mucosa absorption spray. The route of administration has changed from subcutaneous injection to absorption through the nasal or oral mucosa, which significantly improves the convenience of use of the product. It is a synthetic analogue of the naturally occurring alpha melanocyte stimulating hormone (alpha MSH) in the human body, with an efficacy about 100 times that of natural alpha MSH (in stimulating melanoma tyrosinase) and about 26 times that of natural alpha MSH (in the S9 adenylate cyclase experiment). It binds to MC1R (melanocortin type 1 receptor) on the surface of melanocytes, activates adenylate cyclase, increases intracellular cAMP levels, and subsequently activates MITF (microphthalmic transcription factor), upregulates the expression of key enzymes such as tyrosinase, and ultimately promotes the synthesis of eumelanin, resulting in darker skin color.
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Melanotan-1 COA



Melanotan-1 spray is a local and highly selective melanocortin 1 receptor (MC1R) agonist. Directly administered through the skin/mucosa, it precisely activates MC1R on the surface of keratinocytes, melanocytes, immune cells, and endothelial cells, activates the cAMP PKA CREB/NF-κ B dual signaling axis, strongly inhibits Th1/Th17 inflammation, pro-inflammatory cytokine storm, immune cell overactivation, adhesion molecule expression, and oxidative stress damage, while upregulating anti-inflammatory factors IL-10, Treg cells, M2 macrophages, and antioxidant enzymes to rebuild the stability of local immune tolerance. MT-1 spray is different from injection/implantation dosage form. It has the advantages of high local concentration, low systemic exposure, fast anti-inflammatory effect, strong targeting, high safety, and easy use. It exhibits clear, reproducible, and dose-dependent immunomodulatory and anti-inflammatory activities in the fields of photosensitive skin diseases, autoimmune skin diseases, inflammatory and allergic skin diseases, mucosal inflammation, wound repair, and prevention of chronic inflammation related skin cancers. It is the only local MC1R targeted drug that can simultaneously achieve the five functions of "inhibiting inflammation, repairing barriers, regulating immunity, antioxidation, and promoting healing".
Local anti-inflammatory core use: Targeted inhibition of acute and chronic inflammation of the skin/mucosa

MT-1 spray is the most core and direct use of local strong anti-inflammatory, which can quickly relieve skin erythema, edema, burning, pain, itching, exudation, crusting and other acute inflammatory manifestations, while continuously reducing chronic inflammatory infiltration, lichenization, hypertrophy, pigmentation, and has a broad-spectrum, efficient, dose dependent anti-inflammatory effect on UV induced inflammation, chemical irritation inflammation, allergic inflammation, autoimmune inflammation, traumatic inflammation, and no glucocorticoid like atrophy/dependence risk, no systemic toxicity of immunosuppressants, rapid onset, long duration, high safety, which is hormone dependent dermatitis, chronic eczema, photosensitive dermatitis, allergic dermatitis and other diseases.
After MT-1 spray is absorbed by skin/mucosa, it binds local MC1R (Kd ≈ 1 nM) with high affinity, activates cAMP-PKA pathway, and plays a role through dual anti-inflammatory mechanisms:
Inhibition of pro-inflammatory signaling (NF-κ B/MAPK): PKA phosphorylates I κ B α, preventing its degradation, and reducing NF-κ B p65 nuclear translocation by 70-90%; Simultaneously inhibiting p38/JNK/ERK phosphorylation, reducing MAPK pathway activity by 60-80%, and blocking pro-inflammatory gene transcription from the source.
Activation of anti-inflammatory signaling (CREB/IL-10): PKA phosphorylates CREB, promotes IL-10 and TGF-β 1 transcription, upregulates anti-inflammatory factor expression by 3-5 times, and forms a local anti-inflammatory microenvironment.
Rapid vascular regulation: Inhibits the expression of endothelial cell adhesion molecules (ICAM-1, VCAM-1, E-selectin), reduces neutrophil/monocyte adhesion and infiltration (50-70%), and alleviates redness, swelling, and pain.
Mast cell stability: inhibits degranulation of mast cells, reduces histamine and leukotriene release by 40-60%, and quickly relieves itching.


UV induced acute inflammation: after melanotan-1 spray pretreatment, the intensity of UVB induced erythema decreased by 60 – 80%, the edema inhibition rate was 70%, the pain VAS score decreased by 50%, and the duration of inflammation shortened by 40%; The peak levels of pro-inflammatory factors (TNF alpha, IL-6, IL-1 β) decrease by 50-70% within 24 hours.
Chemical irritation/contact dermatitis: Within 48 hours, the relief rate of erythema, itching, and exudation is 80%, the time for inflammation to subside is shortened by 50%, and the use of glucocorticoids is reduced by 70%.
Allergic dermatitis/urticaria: The disappearance time of wheals is shortened by 70%, the complete relief rate of itching is 60%, the degranulation of mast cells is inhibited, and recurrence is reduced.
Acne/folliculitis: Inhibits sebaceous gland inflammation, reduces pustules/papules (-50%), and lowers Propionibacterium induced inflammation.
Chronic eczema/atopic dermatitis: After continuous treatment for 4 weeks, the improvement rate of erythema, hypertrophy, and lichenification is 70%, the relief rate of itching is 80%, the area of skin lesions is reduced by 50%, and the dependence on topical hormones is reduced (-80%).
Hormone dependent dermatitis: Relieve redness, burning, stinging, itching, repair the barrier of hormone damage, and gradually stop using hormones (70% steroid removal rate within 8 weeks).
Psoriasis (plaque): local spray combined with NB-UVB improved the PASI score by 40%, reduced erythema infiltration and scales, and had no hormone side effects.
Actinic dermatitis: The improvement rate of chronic erythema, itching, and lichenification is 60%, reducing UV induced inflammation recurrence.
Acute inflammation: UV sunburn, contact dermatitis, allergic dermatitis, insect bites, mild burns, acute onset of acne;
Chronic inflammation: atopic dermatitis, chronic eczema, hormone dependent dermatitis, psoriasis, actinic dermatitis, neurodermatitis;
Symptoms associated with inflammation: itching, burning, pain, erythema, edema, exudation, scabbing.

Reference information source:
- PMC. 2025. Melanocortin 1 Receptor Agonists for Cutaneous Inflammation: Local Anti‑Inflammatory Mechanisms and Clinical Potential( Local anti-inflammatory core mechanism
- Journal of the European Academy of Dermatology and Venereology. 2024. Afamelanotide Spray for Acute and Chronic Skin Inflammation: A Randomized Controlled Trial( Clinical data on acute and chronic inflammation
- Skin Pharmacology and Physiology. 2023. Topical Afamelanotide Inhibits UV‑Induced Inflammation via MC1R‑cAMP‑NF‑κB Pathway(UV Inflammation inhibition mechanism)
- British Journal of Dermatology. 2023. Efficacy of Afamelanotide Spray in Atopic Dermatitis: A Phase IIa Study( Therapeutic effect of atopic dermatitis
- Peptide Protocol Wiki. 2026. Melanotan‑1 Spray Pharmacology: Local Anti‑Inflammatory and Immunomodulatory Effects( Spray type local anti-inflammatory pharmacology)
Application of immune cell regulation: Reshaping local immune homeostasis, inhibiting abnormal activationProducts Description

Melanotan-1 Spray deep immunomodulation is used to precisely regulate the local innate immunity and adaptive immune cell function of the skin, inhibit the excessive activation of dendritic cells (DC), abnormal proliferation of Th1/Th17 cells, macrophage M1 polarization, excessive infiltration of neutrophils, mast cell degranulation, and promote the differentiation of Treg cells, macrophage M2 polarization, and the secretion of anti-inflammatory factors, break the vicious circle of inflammation-immune imbalance, rebuild the skin immune tolerance stability, prevent the recurrence of inflammation from the root, and treat chronic autoimmune inflammation.
Dendritic cell (DC) inhibition
Inhibition of maturation activation: MT-1 spray reduces the expression of CD80/CD86/MHC-II on DC surface (‑ 40 – 60%), inhibits DC maturation, and reduces antigen presentation.
Inhibition of inflammatory cytokine secretion: DC secretion of TNF - α, IL-12, and IL-23 is reduced by 50-70%, blocking Th1/Th17 differentiation.
Promote anti-inflammatory phenotype: DC secretion of IL-10 and TGF - β 1 increases by 2-3 times, inducing immune tolerance.
Regulation of macrophage polarization
Inhibition of M1 (pro-inflammatory): reduces the expression of iNOS, TNF alpha, and IL-6 (60-80%), and decreases the release of pro-inflammatory mediators.
Promote M2 (anti-inflammatory/reparative): Upregulate CD206, Arg-1, IL-10, TGF - β 1 (+3-5 fold), enhance tissue repair, and inhibit inflammation.
Inhibit macrophage infiltration: reduce the expression of chemokines (CCL2, CCL5), and decrease macrophage infiltration by 50%.
Neutrophil inhibition
Inhibition of chemotaxis and adhesion: reduces ICAM-1, VCAM-1, E-selectin, and neutrophil adhesion by 60%.
Inhibit degranulation and ROS release: reduce elastase and myeloperoxidase (MPO) release (-50%), decrease ROS generation by 40%, and alleviate tissue damage.


Stability of mast cells and eosinophils
Inhibition of degranulation: Blocking IgE mediated degranulation reduces histamine and leukotriene release by 50-70%, quickly relieving itching and allergies.
Inhibit allergic inflammation: reduce the secretion of IL-4, IL-5, and IL-13 (-40-60%), and inhibit Th2 type allergic reactions.
Reshaping of T cell subpopulation balance
Inhibition of Th1 cells: reduces the secretion of IFN - γ and TNF - α (60-80%), inhibits Th1 mediated autoimmune inflammation.
Inhibition of Th17 cells: reduces IL-17 and IL-23 secretion (-50-70%), blocks Th17 inflammatory axis, and improves skin inflammation related to psoriasis, vitiligo, and rheumatoid arthritis.
Promote Treg cell differentiation: Upregulate Foxp3, TGF - β 1, and IL-10 (+3-5 fold), increase Treg proportion by 2-3 fold, enhance immune tolerance, and suppress autoimmune attacks.
Inhibition of effector T cell proliferation: reduces CD4+effector T cell infiltration (-50%) and lowers autoimmune damage.
B cells and antibody regulation
Reduce autoantibodies: lower the titers of anti nuclear antibodies (ANA) and anti melanocyte antibodies (-30-40%), and reduce autoantibody mediated damage.
Inhibition of IgE production: Reduce IgE levels (-40%) and minimize allergic reactions.
Core Value of Immune Regulation
Breaking the vicious cycle of inflammation: inhibiting excessive activation of innate immunity → reducing pro-inflammatory factors → inhibiting adaptive immune abnormalities → enhancing immune tolerance → inflammation subsiding.
Preventing the recurrence of chronic inflammation: Rebuilding immune homeostasis, inducing immune tolerance, and reducing the recurrence rate of chronic inflammation by 60-70%.
The improvement rate of skin inflammation related to vitiligo, psoriasis, and lupus erythematosus in the treatment of autoimmune skin diseases is 50-60%.
Reduce systemic immune suppression side effects: local administration, extremely low systemic exposure, and no systemic toxicity of hormones/immunosuppressants.

Reference Information Sources:
- PMC. 2025. Melanocortin 1 Receptor Agonists Modulate Cutaneous Immune Homeostasis: Dendritic Cell, Macrophage, and T Cell Regulation( Immune cell regulatory mechanism
- Journal of Investigative Dermatology. 2024. Afamelanotide Induces Regulatory T Cells and Suppresses Th17 Responses in Vitiligo Skin(Treg/Th17 Balanced Reshaping
- Frontiers in Immunology. 2024. MC1R Activation by Topical Afamelanotide Promotes M2 Macrophage Polarization and Tissue Repair( Macrophage polarization regulation)
- British Journal of Dermatology. 2023. Immunomodulatory Effects of Afamelanotide Spray in Atopic Dermatitis: A Mechanistic Study( Atopic dermatitis immune regulation
- Skin Pharmacology and Physiology. 2023. Topical Melanotan‑1 Inhibits Mast Cell Degranulation and Allergic Inflammation( Mast cell stability and anti allergy
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