Acetyl-(Nle4,Asp5,D-2-Nal7,Lys10)-cyclo-α-MSH (4-10) amide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SHU 9119 是有效地人类黑皮素受体 3 和 4 (MC3/4R) 拮抗剂，同时也是 MC5R 的部分激动剂，对人类 MC3R, MC4R 和 MC5R 的 IC50 值分别为 0.23, 0.06 和 0.09 nM。

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. 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.

———

———

Others

Other Targets

MC3R;MC4R;MC5R

———

———

168482-23-3

1074.258

C54H71N15O9

>98% (HPLC)

H2O : 10 mg/mL (9.31 mM; ultraphonic)

———

———

(-20℃)

With Ice Pack

≥ 2 years