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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
2 mg | $44 | In Stock | |
5 mg | $68 | In Stock | |
10 mg | $113 | In Stock | |
25 mg | $233 | In Stock | |
50 mg | $396 | In Stock | |
100 mg | $595 | In Stock | |
1 mL x 10 mM (in DMSO) | $77 | In Stock |
Description | EX229 (C991) is an allosteric activator of AMPK, with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1, and α1β2γ1, respectively. |
Targets&IC50 | AMPK α2β1γ1:0.06 μM (Kd), AMPK α1β2γ1:0.51 μM (Kd), AMPK α1β1γ1:0.06 μM (Kd) |
In vitro | Treatment of hepatocytes with EX229 (991) alone results in a slight increase in the phosphorylation of AMPK and RAPTOR only at 0.3 μM, whereas a robust increase in ACC phosphorylation is readily observed and saturated at a concentration of 0.03 μM EX229. AICAR or C13 alone robustly increases T172 phosphorylation of AMPKα, and when 991 is coincubated, there is a modest additional dose-dependent increase in AMPKα phosphorylation. RAPTOR phosphorylation is modestly increased by AICAR or C13 alone, and it is dose-dependently increased when coincubation is carried out with EX229. EX229 also dose-dependently (0.01 and 0.1 μM) inhibits lipogenesis (34% and 63%, respectively), which is further reduced when it is coincubated with a low dose of AICAR (0.03 mM) or C13 (1 μM). Treatment with EX229 promotes dose-dependent increases in ACC and RAPTOR phosphorylation. Similar to the observations in hepatocytes [2]. |
Alias | Compound 991, C991 |
Molecular Weight | 431.87 |
Formula | C24H18ClN3O3 |
Cas No. | 1219739-36-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 12 mg/mL (27.78 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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