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...
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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
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ACLY is ATP citrate lyase, also called ATP-citrate synthase. This record links the verified human identity (NCBI Gene 47; UniProt P53396) to ABMIUM catalogue products.
Biological function: ATP citrate lyase (ACLY) generates cytosolic acetyl-CoA by converting citrate and coenzyme A in an ATP-dependent reaction that also produces oxaloacetate. The acetyl-CoA supplied by ACLY supports pathways including fatty-acid and cholesterol biosynthesis.
