Bempedoic acid, ATP citrate lyase inhibitor (TBI4114)

Description

Product Details

Formal Name: 8-Hydroxy-2,2,14,14-tetramethylpentadecanedioic acid

Alternate Names: ESP 55016; ETC-1002

Molecular Formula: C₁₉H₃₆O₅

Formula Weight: 344.5

CAS Number: 738606-46-7

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

ATP citrate lyase inhibitor

Functions

Inhibitor of ATP citrate lyase (ACL) and activator of AMPK used in the treatment of hypercholesterolemia. In vivo, the active molecule is the CoA ester. Bempedoic acid requires activation by very long-chain acyl-CoA-synthetase (ACSVL1) – the absence of ACSVL1 in skeletal muscle provides a mechanistic basis for its use in statin-intolerant patients. LDL receptor upregulation, decreased LDL-C, and attenuation of atherosclerosis activities are independent of AMPK activation. It significantly cuts the risk of major cardiovascular events. Combination treatment of breast and pancreatic cancer cell lines with bempedoic acid and CDK4/6 inhibitors reduced cell growth and invasion. It displays anti-inflammatory activity possibly through both ACL inhibition and AMPK activation.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.