Bempedoic acid (ETC-1002) mediates inhibition of a wide range of proinflammatory molecules that coincides with the modulation of AMPK and MAP kinase activities. It has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).
In vitro: The phospho-ACC to total-ACC ratio increased by 25% and 60% in cells treated with 50 µM and 100 µM ETC-1002, respectively. Bempedoic acid (ETC-1002) has AMPK-activating properties in primary human MDMs.
In vivo: when mice were treated with 30 mg/kg of Bempedoic acid (ETC-1002) prior to thioglycollate administration, leukocyte influx into the peritoneal cavity was significantly reduced by 48% at 24 h (13.7 × 106/ml lavage fluid; P < 0.008) and by 61% at 72 h (1.8 × 106/ml lavage fluid; P < 0.002)
| Cell Experiment | |
|---|---|
| Cell lines | Primary rat hepatocytes and differentiated human monocyte-derived macrophages |
| Preparation method | Primary rat hepatocytes and differentiated human MDMs are treated with indicated concentrations of ETC-1002 for 12 h. Working solutions of ETC-1002 are prepared in serum-free RPMI 1640 containing 12 mM HEPES, 10,000 U/ml penicillin, and 100 μg/ml streptomycin. |
| Concentrations | 30 μM or 100 μM |
| Incubation time | 12 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6 male mice |
| Formulation | A disodium salt aqueous solution using 2:1 molar ratio of NaOH to ETC-1002 in water containing 0.5% CMC and 0.025% Tween with a final pH 7-8 |
| Dosages | 10 ml/kg |
| Administration | i.p. |
| Molecular Weight | 344.49 |
| Formula | C19H36O5 |
| CAS Number | 738606-46-7 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Nikolic D, et al. Atherosclerosis. ETC-1002: a future option for lipid disorders?
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