Bempedoic acid

SKU: orb1303985

Description

Bempedoic acid (ETC1002) is an oral, once-daily small molecule that lowers LDL-C via hepatic uptake mechanisms distinct from statins, aiming to reduce associated side effects. It is utilized in cardiovascular disease research, with studies demonstrating its efficacy in both in vitro assays and in vivo models of hyperlipidemia.

Research Area

Epigenetics & Chromatin, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 738606-46-7
• MW: 344.49
• Purity: 99.85%
• Formula: C₁₉H₃₆O₅
• SMILES: CC(C)(CCCCCC(O)CCCCCC(C)(C)C(O)=O)C(O)=O
• Target: AMPK,ATP Citrate Lyase
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.81 mM);DMSO:247.5 mg/mL (718.45 mM)

Bioactivity

• 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.
• 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.
• 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)

Storage & Handling

• 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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, ETC 1002, ETC1002, ETC-1002, ESP 55016, ESP55016, ESP-55016, Inhibitor, Bempedoic acid, ATPCitrateLyase, ATP Citrate Lyase, AMPK, AMP-activated protein kinase, ACL, ACLY

Compound Identifiers

PubChem CID

10472693