Size : 10mg
Synonyms: ETC-1002, ETC1002, ETC 1002, ESP-55016
| Description | Bempedoic acid (ETC1002) is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies. Bempedoic acid(ETC1002) is absorbed rapidly in the small intestine and enters the liver through cell surface receptors different from those transporters that selectively take up statins. Bempedoic acid(ETC1002) is a regulator of lipid and carbohydrate metabolism. |
| In vitro | ETC-1002 is an inactivated prodrug that is transformed into its activated form, an ACL inhibitor (activated state, ETC-1002-CoA), through endogenous liver ACS activity in vivo. It inhibits the migration of leukocytes to the peritoneal cavity of mice induced by sulfatide. Additionally, ETC-1002 restores the activity of lipid AMPK and reduces the phosphorylation of JNK in diet-induced obesity mouse models, leading to a decrease in the expression of the macrophage-specific marker 4F/80. |
| In vivo | The mechanism of action of TC-1002 primarily targets two liver enzymes: ATP-citrate lyase (ACL) and AMP-activated protein kinase (AMPK), inhibiting the synthesis of steroids and fatty acids while promoting the oxidation of mitochondrial long-chain fatty acids. ETC-1002 enhances AMPK phosphorylation levels, reduces the activity of MAPKs, and diminishes the production of pro-inflammatory cytokines and chemokines. |
| Synonyms | ETC-1002, ETC1002, ETC 1002, ESP-55016 |
| Kinase Assay | 7.5× compounds are added to a 96-well PolyPlate containing 60 μL of Buffer per well with substrates CoA (200 μM), ATP (400 μM), and [14C]citrate. Reaction is started with 4 μL (300 ng/well) ACL, and the plate is incubated at 37°C for 3 h. Th |
| Cell Research | 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. (Only for Reference) |
| Molecular Weight | 344.49 |
| Formula | C19H36O5 |
| Cas No. | 738606-46-7 |
| Smiles | CC(C)(CCCCCC(O)CCCCCC(C)(C)C(O)=O)C(O)=O |
| Relative Density. | 1.045 g/cm3 (Predicted) |
| Storage | Keep away from moisture,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 247.5 mg/mL (718.45 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.81 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.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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