SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partialMC5Ragonist; withIC₅₀values of 0.23, 0.06, and 0.09 nM for humanMC3R,MC4RandMC5R, 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].

1074.24

Solid

C₅₄H₇₁N₁₅O₉

168482-23-3

Ac-{Nle}-cyclo[Asp-His-D-{Nal}-Arg-Trp-Lys]-NH2

Ac-{Nle}-cyclo[DHD-{Nal}-RWK]-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)

H₂O : 10 mg/mL(9.31 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。