Nonapeptide-1Nonapeptide-1
MedChemExpress (MCE)
HY-P0097
158563-45-2
Melanostatine-5
99.04%
Sealed storage, away from moisture and light Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture and light)
Room temperature in continental US
may vary elsewhere.
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and 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, skin cancer.
Nonapeptide-1 (153N-6) inhibits α-melanocyte hormone (α-MSH)-induced melanosome dispersion, with an IC50 value of 11 nM[1]. 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[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].
MC1R 40 nM (Ki) MC3R 0.47 μM (Ki) MC4R 1.34 μM (Ki) MC5R 2.4 μM (Ki)
Met-Pro-Phe-Arg-Trp-Phe-Lys-Pro-Val-NH2
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[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. [Content Brief]
[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). [Content Brief]
[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. [Content Brief]