Nonapeptide-1 (Melanostatine-5)，一种多肽类激素，是MC1R选择性拮抗剂 (Ki: 40 nM)。 Nonapeptide-1 是一种竞争性的α-MSH拮抗剂，可有效抑制黑素细胞中 α-MSH 诱导的细胞内cAMP和黑素体扩散 (IC50分别为 2.5 nM 和 11 nM)。 Nonapeptide-1 抑制黑色素合成，可用于研究皮肤色素沉着和肾上腺类固醇生成的调节、皮肤癌。
| 生物活性 | Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist ofMC1R(Ki: 40 nM). Nonapeptide-1 is a competitiveα-MSHantagonist that potently inhibits intracellularcAMPand melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skincancer[1][2][3]. |
| IC50& Target[2] | MC1R 40 nM (Ki) | MC3R 0.47 μM (Ki) | MC4R 1.34 μM (Ki) | MC5R 2.4 μM (Ki) |
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体外研究
(In Vitro) | Nonapeptide-1 (153N-6) inhibits α-melanocyte hormone (α-MSH)-induced melanosome dispersion, with an IC50value of 11 nM[1].
Nonapeptide-1 (0.1 nM-1 μΜ, 30 min) inhibits α-MSH-induced intracellular cAMP levels in melanocytes, with an IC50of 2.5 nM[1].
Nonapeptide-1 (153N-6) shows highest affinity for MC1R (Ki: 40 nM) in COS-1 cells expressing human receptors, and is selective for MC1R over MC3R, MC4R, and MC5R (Ki: 0.47, 1.34, and 2.4 μΜ, respectively)[2].
Nonapeptide-1 (N-1A, 20 μΜ, 3 days) inhibits the basal melanin synthesis and reverses UVA-induced melanin increase in Human epidermal melanocytes (HEM cells) and HaCaT cells[3].
Nonapeptide-1 (20 μΜ, 3 days) competes with α-MSH and downregulates the expression of MC1R, tyrosinase, TRP1, TRP2, and MITF via binding to MC1R in HaCaT cells and HEM cells[3].
Western Blot Analysis[3] | Cell Line: | HaCaT cells, Human epidermal melanocytes (HEM) | | Concentration: | 20 μΜ | | Incubation Time: | 3 days | | Result: | Downregulated the expression of MC1R, tyrosinase, TRP1, TRP2, and MITF. |
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| 分子量 | |
| Formula | |
| CAS 号 | |
| Sequence | Met-Pro-Phe-Arg-Trp-Phe-Lys-Pro-Val-NH2 |
| Sequence Shortening | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
