Nonapeptide-1 acetate salt
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1266.56 |
| Molecular Formula | C63H91N15O11S |
| SMILES | - |
1 Publications Citing Use of MCE
Summary
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R ( K i : 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes ( IC 50 : 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, skin cancer [1] [2] [3] .
IC50 & Target
|
MC3R 0.47 μM (Ki) |
MC4R 1.34 μM (Ki) |
MC5R 2.4 μM (Ki) |
In Vitro
Nonapeptide-1 acetate salt (153N-6) inhibits α-melanocyte hormone (α-MSH)-induced melanosome dispersion, with an IC
50
value 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 IC
50
of 2.5 nM
[1]
.
Nonapeptide-1 acetate salt (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 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
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)
Solvent & Solubility
H 2 O : 50 mg/mL ( 39.48 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 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 |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (39.48 mM); Clear solution; Need ultrasonic
References
- [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.
- [2] [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).
- [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.
