SHU-9119 is a potent melanocortin MC3 and MC4 receptor antagonist with IC50 of 0.23 nM and 0.06 nM, respectively.
SHU-9119 also is an MC5R partial agonist (EC50 = 0.12 nM).
SHU-9119 upregulates expression of genes promoting lipogenesis and triglyceride storage (SCD1, LPL, ACCα and FAS), increases triglyceride synthesis and promotes insulin resistance.
SHU-9119 increases food intake, body weight and fat mass when administered centrally in vivo.
Physicochemical Properties
M.Wt
1074.258
Formula
C54H71N15O9
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
Nle(Ac)-cyclo(Asp-His-D-2-Nal-Arg-Trp-Lys)-NH2
References
1. Hruby VJ, et al. J Med Chem. 1995 Sep 1;38(18):3454-61.
2. Fan W, et al. Nature. 1997 Jan 9;385(6612):165-8.
3. Huang QH, et al. J Neurosci. 1997 May 1;17(9):3343-51.
