Acipimox

• CAT Number: A000914
• CAS Number: 51037-30-0
• Molecular Formula: C6H6N2O3
• Molecular Weight: 154.12
• Purity: ≥95%
• Target: Hormone-Sensitive Lipase Inhibitor
• Storage: -20°C
• InChI: 1S/C6H6N2O3/c1-4-2-7-5(6(9)10)3-8(4)11/h2-3H,1H3,(H,9,10)
• InChIKey: DJQOOSBJCLSSEY-UHFFFAOYSA-N
• SMILES: CC1=CN=C(C=[N+]1[O-])C(=O)O

Acipimox, also known as Olbemox and K-9321, is hormone-sensitive lipase inhibitor. Acipimox treatment resulted in a robust elevation in expression of nuclear-encoded mitochondrial gene sets and a mitonuclear protein imbalance, which may indicate activation of the mitochondrial unfolded protein response. Further studies in C2C12 myotubes confirmed a direct effect of acipimox on NAD(+) levels, mitonuclear protein imbalance, and mitochondrial oxidative capacity.

Reference

1: Vestergaard ET, Cichosz SL, Møller N, Jørgensen JOL, Fleischer J. Short-term
acipimox treatment is associated with decreased cardiac parasympathetic
modulation. Br J Clin Pharmacol. 2017 Dec;83(12):2671-2677. doi:
10.1111/bcp.13384. Epub 2017 Aug 24. PubMed PMID: 28736944; PubMed Central PMCID:
PMC5698577.

2: Merovci A, Abdul-Ghani M, Mari A, Solis-Herrera C, Xiong J, Daniele G,
Tripathy D, DeFronzo RA. Effect of Dapagliflozin With and Without Acipimox on
Insulin Sensitivity and Insulin Secretion in T2DM Males. J Clin Endocrinol Metab.
2016 Mar;101(3):1249-56. doi: 10.1210/jc.2015-2597. Epub 2016 Jan 14. PubMed
PMID: 26765576; PubMed Central PMCID: PMC4803159.

3: Makimura H, Stanley TL, Suresh C, De Sousa-Coelho AL, Frontera WR, Syu S,
Braun LR, Looby SE, Feldpausch MN, Torriani M, Lee H, Patti ME, Grinspoon SK.
Metabolic Effects of Long-Term Reduction in Free Fatty Acids With Acipimox in
Obesity: A Randomized Trial. J Clin Endocrinol Metab. 2016 Mar;101(3):1123-33.
doi: 10.1210/jc.2015-3696. Epub 2015 Dec 21. PubMed PMID: 26691888; PubMed
Central PMCID: PMC4803166.

4: van de Weijer T, Phielix E, Bilet L, Williams EG, Ropelle ER, Bierwagen A,
Livingstone R, Nowotny P, Sparks LM, Paglialunga S, Szendroedi J, Havekes B,
Moullan N, Pirinen E, Hwang JH, Schrauwen-Hinderling VB, Hesselink MK, Auwerx J,
Roden M, Schrauwen P. Evidence for a direct effect of the NAD+ precursor acipimox
on muscle mitochondrial function in humans. Diabetes. 2015 Apr;64(4):1193-201.
doi: 10.2337/db14-0667. Epub 2014 Oct 28. PubMed PMID: 25352640; PubMed Central
PMCID: PMC4375076.

5: Nellemann B, Søndergaard E, Jensen J, Pedersen SB, Jessen N, Jørgensen JO,
Nielsen S. Kinetics and utilization of lipid sources during acute exercise and
acipimox. Am J Physiol Endocrinol Metab. 2014 Jul 15;307(2):E199-208. doi:
10.1152/ajpendo.00043.2014. Epub 2014 Jun 3. PubMed PMID: 24895285.

6: Maskali F, Poussier S, Louis H, Boutley H, Lhuillier M, Thornton SN, Karcher
G, Lacolley P, Marie PY. Assessment of the early stage of cardiac remodeling of
spontaneously hypertensive heart failure rats using the quantitative
3-dimensional analysis provided by acipimox-enhanced FDG-PET. Int J Cardiovasc
Imaging. 2014 Feb;30(2):449-56. doi: 10.1007/s10554-013-0350-3. Epub 2014 Jan 3.
PubMed PMID: 24384858.

7: Lindegaard B, Ditlevsen S, Plomgaard P, Mittendorfer B, Pedersen BK. Acute
reduction of lipolysis reduces adiponectin and IL-18: evidence from an
intervention study with acipimox and insulin. Diabetologia. 2013
Sep;56(9):2034-43. doi: 10.1007/s00125-013-2964-3. Epub 2013 Jun 29. PubMed PMID:
23811808; PubMed Central PMCID: PMC3737430.

8: Huang J, Chen R, Wei C, Li R, Yuan G, Liu X, Wang B, Guo R. Pharmacokinetics
and bioequivalence evaluation of two acipimox tablets: a single-dose,
randomized-sequence, two-way crossover study in healthy Chinese male volunteers.
Drug Res (Stuttg). 2013 Feb;63(2):79-83. doi: 10.1055/s-0032-1333228. Epub 2013
Jan 17. PubMed PMID: 23447078.

9: Smitka K, Papezova H, Vondra K, Hill M, Hainer V, Nedvidkova J. Short-term
exercise combined with Acipimox administration induces an increase in plasma ACTH
and its subsequent fall in the recovery phase in bulimic women. Regul Pept. 2013
Mar 10;182:45-52. doi: 10.1016/j.regpep.2012.12.010. Epub 2013 Jan 11. PubMed
PMID: 23318497.

10: Jin F, Jiang S, Yang D, Zhang X, Yang Y, Zhang Y, Li K, Yang Y, Ma S.
Acipimox attenuates atherosclerosis and enhances plaque stability in
ApoE-deficient mice fed a palmitate-rich diet. Biochem Biophys Res Commun. 2012
Nov 9;428(1):86-92. doi: 10.1016/j.bbrc.2012.10.011. Epub 2012 Oct 8. PubMed
PMID: 23058919.