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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $89 | In Stock | In Stock | |
| 5 mg | $383 | In Stock | In Stock | |
| 10 mg | $575 | In Stock | In Stock | |
| 25 mg | $923 | In Stock | In Stock | |
| 50 mg | $1,260 | In Stock | - | |
| 1 mL x 10 mM (in DMSO) | $647 | In Stock | In Stock |
| 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 | MC5R (human):0.09 nM, MC4R (human):0.06 nM, MC3R (human):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 |
| Smiles | CCCC[C@@H](C(N[C@H]1CC(NCCCC[C@@H](C(N)=O)NC([C@@H](NC([C@@H](NC([C@H](NC([C@@H](NC1=O)CC2=CNC=N2)=O)CC3=CC4=CC=CC=C4C=C3)=O)CCCNC(N)=N)=O)CC5=CNC6=C5C=CC=C6)=O)=O)=O)NC(C)=O.CC(O)=O |
| Relative Density. | no data available |
| Sequence | Ac-Nle-DL-Asp(1)-DL-His-D-2Nal-Arg-Trp-Lys(1)-NH2 |
| Sequence Short | XDHXRWK |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (48.49 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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