Nonapeptide-1 (Melanostatine-5) acetate salt，一种多肽类激素，是MC1R选择性拮抗剂 (Ki: 40 nM)。 Nonapeptide-1 acetate salt 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 acetate salt 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) acetate salt, a peptide hormone, is a selective antagonist ofMC1R(Ki: 40 nM). Nonapeptide-1 acetate salt 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 acetate salt 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] | 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 acetate salt (153N-6) inhibits α-melanocyte hormone (α-MSH)-induced melanosome dispersion, with an IC50value of 11 nM[1].
Nonapeptide-1 acetate salt (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 acetate salt (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 acetate salt (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 acetate salt (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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Sealed storage, away from moisture | Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 50 mg/mL(39.48 mM;Need ultrasonic) 配制储备液 | 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 |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
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*以上所有助溶剂都可在本网站选购。 |
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