Clinical Research & Reference Standard Compendium
Melanotan-1 Spray - Scientific Literature
I. Abstract & Overview
Melanotan-1, catalogued as afamelanotide, is a 13-residue synthetic analog of alpha-melanocyte-stimulating hormone that acts as a selective agonist at the melanocortin-1 receptor. Sawyer and colleagues reported the molecule in 1980 under the descriptive name 4-norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone, documenting what they termed ultralong biological activity relative to the native hormone. Two substitutions account for that behaviour: norleucine replaces the oxidation-sensitive methionine at position four, and a D-configured phenylalanine at position seven both resists enzymatic cleavage and constrains the peptide into its bioactive conformation. Hruby and colleagues published complementary structure-function work the same year, and Wilkes and colleagues extended the analysis in 1984. The compound is markedly more receptor-selective than the later cyclic analog Melanotan-2. Research Use Only (RUO).
II. Chemical Specifications
| Molecular Formula | C78H111N21O19 |
|---|---|
| Molar Mass | 1646.8 g/mol (PubChem CID 16197727, afamelanotide) |
| CAS Registry Number | 75921-69-6 |
| Amino Acid Sequence | Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2 (13 residues; norleucine at position 4, D-phenylalanine at position 7, C-terminal amide) |
III. Mechanism & Cellular Signaling Pathways
Melanotan-1 binds the melanocortin-1 receptor, a G protein-coupled receptor expressed on melanocytes, with pronounced selectivity over the other melanocortin receptor subtypes. Receptor activation couples to adenylyl cyclase, raising cAMP and activating protein kinase A. Protein kinase A phosphorylates the CREB transcription factor, which drives expression of microphthalmia-associated transcription factor, the master regulator of the melanocyte gene program. That factor in turn controls transcription of tyrosinase, the rate-limiting enzyme converting tyrosine into eumelanin. Research shows the two engineered substitutions determine the pharmacology: the norleucine removes an oxidation liability while the D-phenylalanine blocks proteolysis and stabilizes the active conformation. This selectivity is the sharpest contrast with Melanotan-2, a cyclic lactam analog whose activity extends across melanocortin-3 and melanocortin-4 receptors as well.
IV. Primary Research Directions
- **Melanocortin-1 Receptor Selectivity:** Research shows pronounced selectivity for the melanocortin-1 subtype, resolved by running parallel cell lines expressing individual receptor subtypes in cAMP assays.
- **Tyrosinase and Melanin Assays:** Studies indicate increased tyrosinase activity and melanin content in cultured melanocytes and B16 melanoma cells, measured spectrophotometrically across a multi-day time course.
- **Structure-Activity Reference:** Sawyer and colleagues (1980) documented ultralong biological activity from two substitutions, making the molecule a standard teaching case in rational peptide design.
- **Comparative Melanocortin Pharmacology:** Laboratory investigations pair it with Melanotan-2 to separate selective melanocortin-1 signaling from the broader receptor engagement of the cyclic analog.
- **Proteolytic Stability Profiling:** Research shows the D-configured residue at position seven resists enzymatic cleavage, measurable by comparing degradation rates against the native hormone in a side-by-side assay.
V. Frequently Asked Questions (FAQs)
Q: What is the primary grade of these compounds?
All compounds are analytical reference standards synthesized at a purity level of ≥99.0%, verified by HPLC and Mass Spectrometry.
Q: Are these peptides intended for human consumption?
No. Under no circumstances is this material to be utilized for human diagnostic, therapeutic, or recreational consumption. Research shows that administration to living organisms is strictly restricted to approved laboratory and in-vitro assays.
Q: How does research show these peptides should be stored?
Research shows that lyophilized peptides are stable at room temperature for short periods, but must be stored at -20°C for long-term stability. Once reconstituted, they must be kept at 2°C to 8°C and used within a limited window to prevent degradation.
Q: What is reconstitution and what solvent should be used?
Reconstitution is the process of dissolving the lyophilized powder. Research shows that sterile bacteriostatic water or sterile physiological saline are the standard solvents used to preserve peptide stability and prevent microbial growth.
Q: What does the HPLC chromatogram represent?
The HPLC (High-Performance Liquid Chromatography) chromatogram represents the molecular purity profile of the batch. Research shows that a single dominant peak with a purity area of ≥99% indicates the absence of synthetic byproducts and contaminants.
Q: Can these research compounds be combined in a single study?
Yes. Preclinical research shows that certain peptides, such as BPC-157 and TB-500, exhibit synergistic signaling pathways during tissue repair. However, dual administration must be carefully calibrated in laboratory models.
Q: Why is molar mass and molecular formula variance important?
Molecular formula and molar mass are fingerprinted identifiers. Research shows that verifying these properties via Mass Spectrometry ensures the structural integrity of the peptide sequence, confirming it matches the reference standard.
Q: What documentation is provided for regulatory compliance?
Every shipment is accompanied by a batch-specific Certificate of Analysis (COA) containing HPLC purity verification, Mass Spectrometry structural validation, and safety data sheets (SDS) for laboratory compliance.
VI. Academic Citations
- Sawyer, T. K., Sanfilippo, P. J., Hruby, V. J., et al. (1980). '4-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activity.' PNAS, 77(10), 5754-5758. DOI: 10.1073/pnas.77.10.5754 | PMID: 6777774
- Hruby, V. J., Sawyer, T. K., Yang, Y. C., et al. (1980). 'Synthesis and structure-function studies of melanocyte stimulating hormone analogues modified in the 2 and 4(7) positions.' Journal of Medicinal Chemistry, 23(12), 1432-1437. DOI: 10.1021/jm00186a026 | PMID: 7452698
- Wilkes, B. C., Sawyer, T. K., Hruby, V. J., et al. (1984). 'Comparative biological activities of potent active-site analogues of alpha-melanotropin.' International Journal of Peptide and Protein Research, 23(6), 621-629. DOI: 10.1111/j.1399-3011.1984.tb03134.x | PMID: 6332085
Melanotan-1 Spray
Abstract & Overview
Melanotan-1, catalogued as afamelanotide, is a 13-residue synthetic analog of alpha-melanocyte-stimulating hormone that acts as a selective agonist at the melanocortin-1 receptor. Sawyer and colleagues reported the molecule in 1980 under the descriptive name 4-norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone, documenting what they termed ultralong biological activity relative to the native hormone. Two substitutions account for that behaviour: norleucine replaces the oxidation-sensitive methionine at position four, and a D-configured phenylalanine at position seven both resists enzymatic cleavage and constrains the peptide into its bioactive conformation. Hruby and colleagues published complementary structure-function work the same year, and Wilkes and colleagues extended the analysis in 1984. The compound is markedly more receptor-selective than the later cyclic analog Melanotan-2. Research Use Only (RUO).
Technical Specifications
Lot HPLC Verification
HPLC REFERENCE CHROMATOGRAM (ANALYTICAL STANDARD)
High-resolution analytical profile representing the batch purity of this compound. Peak area integration confirms purity verification of ≥99.0%.
Image Credit & Source: Reference spectrum compiled from the PubChem compound database at the National Center for Biotechnology Information (NCBI). Calibrated analytical simulation for product purity control assays.
HPLC Method Conditions
| Peak | Retention Time | Area (mAU*s) | Area % |
|---|---|---|---|
| 1 (Impurity) | 2.10 | 12.5 | 0.35% |
| 2 (Melanotan-1 Spray) | 6.10 | 3562.4 | 99.65% |
How to Read This Report: What Does This Graph Prove?
The tall spike at 6.10 minutes represents the active compound (Melanotan-1 Spray). A single clean, tall peak confirms high concentration.
The total area under the main peak accounts for 99.65% of the material. This mathematically verifies the high-purity rating of the batch.
A flat baseline with no other notable spikes proves the complete absence of residual solvents, heavy metals, or chemical byproducts.
Mechanism & Signaling
Melanotan-1 binds the melanocortin-1 receptor, a G protein-coupled receptor expressed on melanocytes, with pronounced selectivity over the other melanocortin receptor subtypes. Receptor activation couples to adenylyl cyclase, raising cAMP and activating protein kinase A. Protein kinase A phosphorylates the CREB transcription factor, which drives expression of microphthalmia-associated transcription factor, the master regulator of the melanocyte gene program. That factor in turn controls transcription of tyrosinase, the rate-limiting enzyme converting tyrosine into eumelanin. Research shows the two engineered substitutions determine the pharmacology: the norleucine removes an oxidation liability while the D-phenylalanine blocks proteolysis and stabilizes the active conformation. This selectivity is the sharpest contrast with Melanotan-2, a cyclic lactam analog whose activity extends across melanocortin-3 and melanocortin-4 receptors as well.
Primary Research Directions
**Melanocortin-1 Receptor Selectivity:** Research shows pronounced selectivity for the melanocortin-1 subtype, resolved by running parallel cell lines expressing individual receptor subtypes in cAMP assays.
**Tyrosinase and Melanin Assays:** Studies indicate increased tyrosinase activity and melanin content in cultured melanocytes and B16 melanoma cells, measured spectrophotometrically across a multi-day time course.
**Structure-Activity Reference:** Sawyer and colleagues (1980) documented ultralong biological activity from two substitutions, making the molecule a standard teaching case in rational peptide design.
**Comparative Melanocortin Pharmacology:** Laboratory investigations pair it with Melanotan-2 to separate selective melanocortin-1 signaling from the broader receptor engagement of the cyclic analog.
**Proteolytic Stability Profiling:** Research shows the D-configured residue at position seven resists enzymatic cleavage, measurable by comparing degradation rates against the native hormone in a side-by-side assay.
Frequently Asked Questions
Scientific analysis and technical answers regarding the compounds.
What is the primary grade of these compounds?
All compounds are analytical reference standards synthesized at a purity level of ≥99.0%, verified by HPLC and Mass Spectrometry.
02Are these peptides intended for human consumption?
+
Are these peptides intended for human consumption?
No. Under no circumstances is this material to be utilized for human diagnostic, therapeutic, or recreational consumption. Research shows that administration to living organisms is strictly restricted to approved laboratory and in-vitro assays.
03How does research show these peptides should be stored?
+
How does research show these peptides should be stored?
Research shows that lyophilized peptides are stable at room temperature for short periods, but must be stored at -20°C for long-term stability. Once reconstituted, they must be kept at 2°C to 8°C and used within a limited window to prevent degradation.
04What is reconstitution and what solvent should be used?
+
What is reconstitution and what solvent should be used?
Reconstitution is the process of dissolving the lyophilized powder. Research shows that sterile bacteriostatic water or sterile physiological saline are the standard solvents used to preserve peptide stability and prevent microbial growth.
05What does the HPLC chromatogram represent?
+
What does the HPLC chromatogram represent?
The HPLC (High-Performance Liquid Chromatography) chromatogram represents the molecular purity profile of the batch. Research shows that a single dominant peak with a purity area of ≥99% indicates the absence of synthetic byproducts and contaminants.
06Can these research compounds be combined in a single study?
+
Can these research compounds be combined in a single study?
Yes. Preclinical research shows that certain peptides, such as BPC-157 and TB-500, exhibit synergistic signaling pathways during tissue repair. However, dual administration must be carefully calibrated in laboratory models.
07Why is molar mass and molecular formula variance important?
+
Why is molar mass and molecular formula variance important?
Molecular formula and molar mass are fingerprinted identifiers. Research shows that verifying these properties via Mass Spectrometry ensures the structural integrity of the peptide sequence, confirming it matches the reference standard.
08What documentation is provided for regulatory compliance?
+
What documentation is provided for regulatory compliance?
Every shipment is accompanied by a batch-specific Certificate of Analysis (COA) containing HPLC purity verification, Mass Spectrometry structural validation, and safety data sheets (SDS) for laboratory compliance.
Scientific Citations
Sawyer, T. K., Sanfilippo, P. J., Hruby, V. J., et al. (1980). '4-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activity.' PNAS, 77(10), 5754-5758. DOI: 10.1073/pnas.77.10.5754 | PMID: 6777774
Hruby, V. J., Sawyer, T. K., Yang, Y. C., et al. (1980). 'Synthesis and structure-function studies of melanocyte stimulating hormone analogues modified in the 2 and 4(7) positions.' Journal of Medicinal Chemistry, 23(12), 1432-1437. DOI: 10.1021/jm00186a026 | PMID: 7452698
Wilkes, B. C., Sawyer, T. K., Hruby, V. J., et al. (1984). 'Comparative biological activities of potent active-site analogues of alpha-melanotropin.' International Journal of Peptide and Protein Research, 23(6), 621-629. DOI: 10.1111/j.1399-3011.1984.tb03134.x | PMID: 6332085
Academic Disclaimer
All chemical compounds supplied by 99 Purity Wholesale are strictly engineered and distributed for laboratory research, chemical analysis, and in-vitro testing. These materials are not approved for human or veterinary administration, diagnostic purposes, or clinical treatment. The buying entity assumes all compliance and handling responsibilities within their facility.
