Nonapeptide-1

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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 can inhibit the synthesis of melanin which makes it of interest for treating certain skin conditions.?

Nonapeptide-1 (153N-6) inhibits α-melanocyte hormone (α-MSH)-induced melanosome dispersion, with an IC50 value of 11 nM.Nonapeptide-1 (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 (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 (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 (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. Western Blot Analysis 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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Met-Pro-D-Phe-Arg-D-Trp-Phe-Lys-Pro-Val- | Melanostatine 5

Others

Other Targets

Others

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158563-45-2

1206.5

C61H87N15O9S

>98% (HPLC)

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CSCCC(N)C(=O)N1CCCC1C(=O)NC(Cc1ccccc1)C(=O)NC(CCCNC(=N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCCN)C(=O)N1CCCC1C(=O)NC(C(N)=O)C(C)C

(S)-1-(L-methionyl)-N-((R)-1-(((S)-1-(((R)-1-(((S)-1-(((S)-6-amino-1-((S)-2-(((S)-1-amino-3-methyl-1-oxobutan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-oxohexan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)amino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)pyrrolidine-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years