Bempedoic acid [738606-46-7]

Katalog-Nummer T3625-500mg

Size : 500mg

Marke : TargetMol


Bempedoic acid

(Synonyms: ETC-1002, ETC1002, ETC 1002, ESP-55016) Copy Product Info
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.
Bempedoic acid
Cas No. 738606-46-7
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.94%
Color:White

Product Introduction

Bioactivity
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.
SynonymsETC-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)
Chemical Properties
Molecular Weight344.49
FormulaC19H36O5
Cas No.738606-46-7
SmilesCC(C)(CCCCCC(O)CCCCCC(C)(C)C(O)=O)C(O)=O
Relative Density.1.045 g/cm3 (Predicted)
Storage & Solubility Information
StorageKeep 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
1mg5mg10mg50mg
1 mM2.9028 mL14.5142 mL29.0284 mL145.1421 mL
5 mM0.5806 mL2.9028 mL5.8057 mL29.0284 mL
10 mM0.2903 mL1.4514 mL2.9028 mL14.5142 mL
20 mM0.1451 mL0.7257 mL1.4514 mL7.2571 mL
50 mM0.0581 mL0.2903 mL0.5806 mL2.9028 mL
100 mM0.0290 mL0.1451 mL0.2903 mL1.4514 mL
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.