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MCE 国际站:Nonapeptide-1 acetate salt
产品活性: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。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Melanocortin Receptor
In Vitro: Nonapeptide-1 acetate salt (153N-6) inhibits α-melanocyte hormone (α-MSH)-induced melanosome dispersion, with an IC50 value of 11 nM.
Nonapeptide-1 acetate salt (0.1 nM-1 μΜ, 30 min) inhibits α-MSH-induced intracellular cAMP levels in melanocytes, with an IC50 of 2.5 nM.
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).
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.
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.
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