melanocortin MC3 and MC4 receptor antagonist
CAS：168482-23-3
分子式：C54H71N15O9
分子量：1074.25
纯度：98%
存储：Store at -20°C

Background:

SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
Blockade of CNS-Mcr via chronic intracerebroventricular infusion of SHU9119 (24 nmol/d for 7 days) increases food intake in ad libitum-fed rats compared with control. Weight gain of SHU9119 treated rats is significantly higher than control. SHU9119 treatment potently increases metabolic efficiency. SHU9119 markedly increases mRNA levels of genes promoting lipogenesis and TAG storage in adipocytes, including stearoyl-CoA desaturase-1, lipoprotein lipase, acetyl-CoA carboxylase α, and fatty acid synthase[2]. SHU9119 increases food intake (+30%) and body fat (+50%) and decreases EE by reduction in fat oxidation (?42%). In addition, SHU9119 impairs the uptake of VLDL-TG by BAT. In line with this, SHU9119 decreases uncoupling protein-1 levels in BAT (?60%) and induces large intracellular lipid droplets, indicative of severely disturbed BAT activity[3]
Reference:
[1]. Grieco P, et al. Further structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. Peptides. 2007 Jun;28(6):1191-6.
[2]. Nogueiras R, et al. The central melanocortin system directly controls peripheral lipid metabolism. J Clin Invest. 2007 Nov;117(11):3475-88.
[3]. Kooijman S, et al. Inhibition of the central melanocortin system decreases brown adipose tissue activity. J Lipid Res. 2014 Oct;55(10):2022-32.