Nonapeptide-1  (Synonyms: Melanostatine-5)

Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (K_i: 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^[1][2][3].

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 (K_i: 40 nM) in COS-1 cells expressing human receptors, and is selective for MC1R over MC3R, MC4R, and MC5R (K_i: 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1206.50

C₆₁H₈₇N₁₅O₉S

158563-45-2

Solid

White to off-white

Met-Pro-Phe-Arg-Trp-Phe-Lys-Pro-Val-NH2

MPFRWFKPV-NH2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [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]