Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
MC1R MC3R 0.47 μM (Ki) MC4R 1.34 μM (Ki) MC5R 2.4 μM (Ki)
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ln Vitro |
Nonapeptide-1 acetate salt(153N-6) has an IC50 value of 11 nM and inhibits the dispersion of melanosomes caused by α-melanocyte hormone (α-MSH). Melanocytes exposed to α-MSH-induced intracellular cAMP levels are inhibited by nonapeptide-1 acetate salt (0.1 nM-1 μM, 30 min), with an IC50 of 2.5 nM[1]. Nonapeptide-1 acetate salt (153N-6) is preferential for MC1R over MC3R, MC4R, and MC5R (Ki: 0.47, 1.34, and 2.4 μM, respectively) and has the highest affinity for MC1R (Ki: 40 nM) in COS-1 cells expressing human receptors[2]. Human epidermal melanocytes (HEM cells) and HaCaT cells are treated with nonapeptide-1 acetate salt (N-1A, 20 μM, 3 days) to decrease basal melanin synthesis and reverse UVA-induced melanin increase[3]. Nonapeptide-1 acetate salt (20 μM, 3 days) binds to MC1R in HaCaT and HEM cells, competing with α-MSH to downregulate the expression of MC1R, tyrosinase, TRP1, TRP2, and MITF[3].
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Cell Assay |
Western Blot Analysis[3]
Cell Types: HaCaT cells, Human epidermal melanocytes(HEM) Tested Concentrations: 20 μΜ Incubation Duration: 3 days Experimental Results: Downregulated the expression of MC1R, tyrosinase, TRP1, TRP2, and MITF. |
References |
[1]. Jayawickreme CK, et al. Discovery and structure-function analysis of alpha-melanocyte-stimulating hormone antagonists. J Biol Chem. 1994 Nov 25;269(47):29846-54.
[2]. [2] Schiöth, H.B., et al. Characterization of the binding of MSH-B, HB-228, GHRP-6 and 153N-6 to the human melanocortin receptor subtypes. Neuropeptides 31(6), 565-571 (1997). [3]. Jiaoquan Chen, et al. Effects of tea polyphenols on UVA-induced melanogenesis via inhibition of α-MSH-MC1R signalling pathway. Postepy Dermatol Alergol. 2022 Apr;39(2):327-335. |
Molecular Formula |
C63H91N15O11S
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Molecular Weight |
1266.56
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Related CAS # |
Nonapeptide-1;158563-45-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
H2O :~50 mg/mL (~39.48 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (39.48 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.7895 mL | 3.9477 mL | 7.8954 mL | |
5 mM | 0.1579 mL | 0.7895 mL | 1.5791 mL | |
10 mM | 0.0790 mL | 0.3948 mL | 0.7895 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.