Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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.
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. |
Targets&IC50 | hMC5R:0.09 nM, hMC4R:0.06 nM, hMC3R:0.23 nM |
In vivo | Compared with control, blocking CNS-Mcr by chronic intracerebroventricular infusion of SHU9119 (24 nmol/d for 7 days) increases food intake in ad libitum-fed rats. Weight gain of SHU9119 treated rats is significantly higher than control. SHU9119 treatment effectively 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%). Furthermore, 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. |
Synonyms | SHU 9119 acetate (168482-23-3 free base) |
Molecular Weight | 1134.29 |
Formula | C56H75N15O11 |
CAS No. | T16879L |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 55 mg/ml (48.49 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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SHU 9119 acetate T16879L G蛋白偶联受体 神经科学 Melanocortin Receptor SHU 9119 acetate (168482-23-3 free base) Inhibitor inhibitor inhibit