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738606-46-7-Bempedoic acid Bempedoic acid

Bempedoic acid

For research use only. Not for therapeutic Use.

  • CAT Number: I004743
  • CAS Number: 738606-46-7
  • Molecular Formula: C₁₉H₃₆O₅
  • Molecular Weight: 344.49
  • Purity: 98%
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Related products: Terpinyl Acetate     Demethyleneberberine     Efetaal    
Research Areas: Lipid Lowering    

Bempedoic acid (Cat No.:I004743) is indeed a novel, first-in-class, an orally available small molecule that lowers LDL-C levels. It functions as an activator of hepatic AMP-activated protein kinase (AMPK), which plays a key role in cellular energy regulation. Activation of AMPK by bempedoic acid leads to increased fatty acid oxidation and reduced cholesterol synthesis in the liver. Additionally, bempedoic acid exhibits potent inhibitory activity against hepatic ATP-citrate lyase, an enzyme involved in the production of cholesterol and fatty acids. These dual mechanisms of action contribute to the LDL-C-lowering effects of bempedoic acid, making it a promising therapeutic option for patients with hypercholesterolemia.


Catalog Number I004743
CAS Number 738606-46-7
Synonyms

8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid

Molecular Formula C₁₉H₃₆O₅
Purity 98%
Target ACLY
Target Protein

P53396

Solubility 10 mM in DMSO
Appearance Solid
Storage Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
Overview of Clinical Research

<span style=”color:#000000;”><span style=”font-size:12px;”><span style=”font-family:arial,helvetica,sans-serif;”>Bempedoic acid is an&nbsp;AMP activated protein kinase stimulant and a ATP citrate (pro S) lyase inhibitor. It was registered for Hypercholesterolaemia in Switzerland (PO) in Dec 2020.</span></span></span>
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IC50 IC50:29 μM(ACL inhibitor)
IUPAC Name 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid
InChI InChI=1S/C19H36O5/c1-18(2,16(21)22)13-9-5-7-11-15(20)12-8-6-10-14-19(3,4)17(23)24/h15,20H,5-14H2,1-4H3,(H,21,22)(H,23,24)
InChIKey HYHMLYSLQUKXKP-UHFFFAOYSA-N
SMILES CC(C)(CCCCCC(CCCCCC(C)(C)C(=O)O)O)C(=O)O
Reference

<br />
1:Bempedoic Acid (ETC-1002): an Investigational Inhibitor of ATP Citrate Lyase. Bilen O, Ballantyne CM.Curr Atheroscler Rep. 2016 Oct;18(10):61. Review. PMID: 27663902 Free PMC Article<br />
2:Treatment with ETC-1002 alone and in combination with ezetimibe lowers LDL cholesterol in hypercholesterolemic patients with or without statin intolerance. Thompson PD, MacDougall DE, Newton RS, Margulies JR, Hanselman JC, Orloff DG, McKenney JM, Ballantyne CM.J Clin Lipidol. 2016 May-Jun;10(3):556-67. doi: 10.1016/j.jacl.2015.12.025. Epub 2016 Jan 6. PMID: 27206943 Free Article<br />
3:Effect of ETC-1002 on Serum Low-Density Lipoprotein Cholesterol in Hypercholesterolemic Patients Receiving Statin Therapy. Ballantyne CM, McKenney JM, MacDougall DE, Margulies JR, Robinson PL, Hanselman JC, Lalwani ND.Am J Cardiol. 2016 Jun 15;117(12):1928-33. doi: 10.1016/j.amjcard.2016.03.043. Epub 2016 Apr 6. PMID: 27138185 Free Article<br />
4:Use of ETC-1002 to treat hypercholesterolemia in patients with statin intolerance. Thompson PD, Rubino J, Janik MJ, MacDougall DE, McBride SJ, Margulies JR, Newton RS.J Clin Lipidol. 2015 May-Jun;9(3):295-304. doi: 10.1016/j.jacl.2015.03.003. Epub 2015 Mar 19. PMID: 26073387 Free Article<br />
5:ETC-1002: a future option for lipid disorders? Nikolic D, Mikhailidis DP, Davidson MH, Rizzo M, Banach M.Atherosclerosis. 2014 Dec;237(2):705-10. doi: 10.1016/j.atherosclerosis.2014.10.099. Epub 2014 Oct 31. Review. PMID: 25463109<br />
6:Efficacy and safety of ETC-1002, a novel investigational low-density lipoprotein-cholesterol-lowering therapy for the treatment of patients with hypercholesterolemia and type 2 diabetes mellitus. Gutierrez MJ, Rosenberg NL, Macdougall DE, Hanselman JC, Margulies JR, Strange P, Milad MA, McBride SJ, Newton RS.Arterioscler Thromb Vasc Biol. 2014 Mar;34(3):676-83. doi: 10.1161/ATVBAHA.113.302677. Epub 2014 Jan 2. PMID: 24385236 Free Article<br />
7:ETC-1002 regulates immune response, leukocyte homing, and adipose tissue inflammation via LKB1-dependent activation of macrophage AMPK. Filippov S, Pinkosky SL, Lister RJ, Pawloski C, Hanselman JC, Cramer CT, Srivastava RA, Hurley TR, Bradshaw CD, Spahr MA, Newton RS.J Lipid Res. 2013 Aug;54(8):2095-108. doi: 10.1194/jlr.M035212. Epub 2013 May 24. PMID: 23709692 Free PMC Article<br />
8:AMP-activated protein kinase and ATP-citrate lyase are two distinct molecular targets for ETC-1002, a novel small molecule regulator of lipid and carbohydrate metabolism. Pinkosky SL, Filippov S, Srivastava RA, Hanselman JC, Bradshaw CD, Hurley TR, Cramer CT, Spahr MA, Brant AF, Houghton JL, Baker C, Naples M, Adeli K, Newton RS.J Lipid Res. 2013 Jan;54(1):134-51. doi: 10.1194/jlr.M030528. Epub 2012 Nov 1. PMID: 23118444 Free PMC Article

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