| Description | SHU 9119 acetate is a well-known antagonist of human melanocortin 3 and 4 (hMC3R, hMC4R) receptors and a partial hMC5R agonist. The IC50 values of human MC3R, MC4R and MC5R is 0.23, 0.06, and 0.09 nM respectively. |
| In vivo | 与对照组相比，通过慢性脑室内灌注SHU9119（24nM/天，持续7天）阻断CNS-Mcr，可增加自由进食大鼠的食物摄入量。SHU9119处理的大鼠体重增加显著高于对照组。SHU9119治疗有效提高了代谢效率。SHU9119显著增加了促进脂肪生成和三酰甘油（TAG）储存的基因的mRNA水平，包括硬脂酰-CoA去饱和酶-1、脂蛋白脂酶、乙酰-CoA羧化酶α和脂肪酸合成酶。SHU9119增加食物摄入量（+30%）和体脂肪（+50%），并通过减少脂肪氧化（约42%）降低能量消耗（EE）。此外，SHU9119降低了棕色脂肪组织（BAT）对VLDL-TG的摄取。与此同时，SHU9119降低了BAT中解耦联蛋白-1的水平（约60%），并诱导了大型的细胞内脂滴形成，这表明BAT活动受到了严重干扰。 |
| Target activity | MC4R (human):0.06 nM, MC3R (human):0.23 nM, MC5R (human):0.09 nM |
| Synonyms | SHU 9119 acetate (168482-23-3 free base) |
| molecular weight | 1134.29 |
| Molecular formula | C56H75N15O11 |
| Storage | keep away from moisture|Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/ml (48.49 mM) |
| References | 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 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. |