货号	规格	价格	上海	北京	珠海	重庆	武汉
S83859-1mg买3赠1	99.70%	￥630.00 S83859-1mg ￥630.00 现货（买3赠1）	9 9	-	-	-	-
S83859-5mg买3赠1	99.70%	￥2540.00 S83859-5mg ￥2540.00 现货（买3赠1）	8 8	-	-	-	-
S83859-25mg	99.70%	￥10000.00 S83859-25mg ￥10000.00 现货	5 5	-	-	-	-

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产品描述：

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.

靶点：

MC3R;MC4R;MC5R;Others

体内研究：

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

参考文献：

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.

溶解性：

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

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	0.931 ml	4.654 ml	9.309 ml
5 mM	0.186 ml	0.931 ml	1.862 ml
10 mM	0.093 ml	0.465 ml	0.931 ml
50 mM	0.019 ml	0.093 ml	0.186 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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