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SHU 9119 is an effective human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist (IC50: 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively).
SHU 9119 is an effective human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist (IC50: 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively).
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 μg | ¥ 1,340 | 35日内发货 | |
1 mg | ¥ 2,110 | 35日内发货 |
产品描述 | SHU 9119 is an effective human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist (IC50: 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively). |
靶点活性 | MC5R:0.23 nM, MC3R:0.23 nM, MC4R:0.23 nM |
体内活性 | 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. The 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 increases food intake (+30%) and body fat (+50%) and decreases EE by a reduction in fat oxidation (?42%). SHU9119 impairs the uptake of VLDL-TG by BAT. SHU9119 reduces uncoupling protein-1 levels in BAT (?60%) and induces large intracellular lipid droplets, indicative of severely disturbed BAT activity [2][3]. |
分子量 | 1074.258 |
分子式 | C54H71N15O9 |
CAS No. | 168482-23-3 |
密度 | 1.43 g/cm3 |
存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | H2O: 20 mg/mL (18.62 mM), Sonication is recommended. | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
H2O
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