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Chemical Compound Review

Ibrolipim     N-(4-bromo-2-cyano-phenyl)- 4...

Synonyms: OPF-009, CHEMBL34234, AG-D-67631, ACMC-20ejl0, NO-1886, ...
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Disease relevance of NO 1886


High impact information on NO 1886


Chemical compound and disease context of NO 1886


Biological context of NO 1886


Anatomical context of NO 1886

  • In summary, the results of our study indicate that compound NO-1886 increases LPL activity, causing an elevation in HDL levels, and that long-term administration of NO-1886 to rats with experimental atherosclerosis provides significant protection against the development of coronary artery lesions [1].
  • In myocardium and skeletal muscle a high-fat diet lowered lipoprotein lipase activity, an effect lessened by NO-1886 [4].
  • A similar pattern existed for fat accumulation [visceral fat (g): chow, 35.9 +/- 3.2; high-fat, 81.9 +/- 6.6; high-fat + NO-1886, 52.3 +/- 4.7, p < 0.01 high-fat vs the other groups] [4].
  • NO-1886 attenuated smooth muscle contraction induced by the cumulative addition of CaCl(2) [11].
  • NO-1886 decreases ectopic lipid deposition and protects pancreatic beta cells in diet-induced diabetic swine [12].

Associations of NO 1886 with other chemical compounds

  • Following our report that administration of 4-diethoxyphosphorylmethyl-N-(4-bromo-2-cyanophenyl) benzamide (NO-1886) to rats elevated postheparin lipoprotein lipase (LPL) activity through an increase in the enzyme mass, we now investigate antiatherogenic effects of NO-1886 in cholesterol-fed New Zealand White rabbits [13].
  • Eadie-Hofstee plots of phosphonate O-deethylation of NO-1886 in human liver microsomes showed a biphasic curve, indicating low- and high-K(m) components [10].
  • However, NO-1886 affected steroid production from adrenocortical cells in rats, dogs, monkeys, and humans in in vitro studies [14].
  • The results show that administration of NO-1886 attenuated aortic contraction induced by phenylephrine and/or a high K(+) environment, in both the presence and absence of aortic endothelium [11].
  • The endothelium-dependent relaxation of the thoracic aorta caused by histamine was significantly impaired in old rats (% relaxation at 10(-5.5) M histamine: young rats 25.4+/-3.1%; old rats 14.1+/-1.9%, P < 0.01), an effect completely prevented by NO-1886 (old rats + NO-1886; 22.8+/-2.8%, P < 0.05 vs. old rats) [15].

Gene context of NO 1886

  • Recombinant CYP3A4 and CYP2C8 expressed in baculovirus-infected insect cells and human lymphoblastoid cells exhibited a high activity for phosphonate O-deethylation of NO-1886 [10].
  • Following additional culture for 24 hr in fresh medium without NO-1886, the expression of CYP3A4 mRNA was comparable to that in controls [16].
  • However, the CYP3A5 mRNA level after exposure to 50 microM NO-1886 was not significantly increased [17].
  • The expression levels of CYP1A2, CYP2B2, CYP2C12, and CYP2E1 mRNA in primary cultures of rat hepatocytes were not affected by exposure to NO-1886 at 2, 10, or 50 microM [16].
  • A higher concentration (50 microM) of NO-1886 induced an increase in CYP2C8 mRNA and a decrease in CYP2C19 mRNA, and these changes continued after additional culture for 24 hr in fresh medium without NO-1886 [16].

Analytical, diagnostic and therapeutic context of NO 1886


  1. The novel compound NO-1886 increases lipoprotein lipase activity with resulting elevation of high density lipoprotein cholesterol, and long-term administration inhibits atherogenesis in the coronary arteries of rats with experimental atherosclerosis. Tsutsumi, K., Inoue, Y., Shima, A., Iwasaki, K., Kawamura, M., Murase, T. J. Clin. Invest. (1993) [Pubmed]
  2. Concurrent suppression of hyperlipidemia and intestinal polyp formation by NO-1886, increasing lipoprotein lipase activity in Min mice. Niho, N., Mutoh, M., Takahashi, M., Tsutsumi, K., Sugimura, T., Wakabayashi, K. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  3. Correction of hypertriglyceridemia with low high-density lipoprotein cholesterol by the novel compound NO-1886, a lipoprotein lipase-promoting agent, in STZ-induced diabetic rats. Tsutsumi, K., Inoue, Y., Shima, A., Murase, T. Diabetes (1995) [Pubmed]
  4. The lipoprotein lipase activator, NO-1886, suppresses fat accumulation and insulin resistance in rats fed a high-fat diet. Kusunoki, M., Hara, T., Tsutsumi, K., Nakamura, T., Miyata, T., Sakakibara, F., Sakamoto, S., Ogawa, H., Nakaya, Y., Storlien, L.H. Diabetologia (2000) [Pubmed]
  5. NO-1886 upregulates ATP binding cassette transporter A1 and inhibits diet-induced atherosclerosis in Chinese Bama minipigs. Zhang, C., Yin, W., Liao, D., Huang, L., Tang, C., Tsutsumi, K., Wang, Z., Liu, Y., Li, Q., Hou, H., Cai, M., Xiao, J. J. Lipid Res. (2006) [Pubmed]
  6. Effect of the lipoprotein lipase activator NO-1886 on adriamycin-induced nephrotic syndrome in rats. Nakayama, K., Hara, T., Kusunoki, M., Tsutsumi, K., Minami, A., Okada, K., Sakamoto, S., Ohnaka, M., Miyata, T., Nakamura, T., Aoki, T., Fukatsu, A., Nakaya, Y., Kakumu, S. Metab. Clin. Exp. (2000) [Pubmed]
  7. Lipoprotein lipase activator NO-1886 improves fatty liver caused by high-fat feeding in streptozotocin-induced diabetic rats. Kusunoki, M., Tsutsumi, K., Inoue, Y., Hara, T., Miyata, T., Nakamura, T., Ogawa, H., Sakakibara, F., Fukuzawa, Y., Okabayashi, N., Kato, K., Ikeda, H., Kurokawa, T., Ishikawa, T., Otake, K., Nakaya, Y. Metab. Clin. Exp. (2004) [Pubmed]
  8. Effect of lipoprotein lipase activators bezafibrate and NO-1886, on B16 melanoma-induced cachexia in mice. Kawamura, I., Yamamoto, N., Sakai, F., Yamazaki, H., Goto, T. Anticancer Res. (1999) [Pubmed]
  9. Synthesis and hypolipidemic activities of novel 2-[4-[diethoxyphosphoryl)methyl]phenyl]quinazolines and 4(3H)-quinazolinones. Kurogi, Y., Inoue, Y., Tsutsumi, K., Nakamura, S., Nagao, K., Yoshitsugu, H., Tsuda, Y. J. Med. Chem. (1996) [Pubmed]
  10. Phosphonate O-deethylation of [4-(4-bromo-2-cyano-phenylcarbamoyl) benzyl]-phosphonic acid diethyl ester, a lipoprotein lipase-promoting agent, catalyzed by cytochrome P450 2C8 and 3A4 in human liver microsomes. Morioka, Y., Otsu, M., Naito, S., Imai, T. Drug Metab. Dispos. (2002) [Pubmed]
  11. NO-1886, a lipoprotein lipase activator, attenuates vascular smooth muscle contraction in rat aorta. Nakamura, A., Harada, N., Takahashi, A., Mawatari, K., Nakano, M., Tsutsumi, K., Nakaya, Y. Eur. J. Pharmacol. (2007) [Pubmed]
  12. NO-1886 decreases ectopic lipid deposition and protects pancreatic beta cells in diet-induced diabetic swine. Yin, W., Liao, D., Kusunoki, M., Xi, S., Tsutsumi, K., Wang, Z., Lian, X., Koike, T., Fan, J., Yang, Y., Tang, C. J. Endocrinol. (2004) [Pubmed]
  13. Antiatherogenic effects of a novel lipoprotein lipase-enhancing agent in cholesterol-fed New Zealand white rabbits. Chiba, T., Miura, S., Sawamura, F., Uetsuka, R., Tomita, I., Inoue, Y., Tsutsumi, K., Tomita, T. Arterioscler. Thromb. Vasc. Biol. (1997) [Pubmed]
  14. Lipoprotein lipase promoting agent, NO-1886, modulates adrenal functions: species difference in effects of NO-1886 on steroidogenesis. Shimono, K., Tsutsumi, K., Yaguchi, H., Omura, M., Sasano, H., Nishikawa, T. Steroids (1999) [Pubmed]
  15. A lipoprotein lipase activator, NO-1886, improves endothelium-dependent relaxation of rat aorta associated with aging. Hara, T., Kusunoki, M., Tsutsumi, K., Okada, K., Sakamoto, S., Ohnaka, M., Nakamura, T., Miyata, T., Nakayama, K., Fukatsu, A., Kato, K., Kakumu, S., Nakaya, Y. Eur. J. Pharmacol. (1998) [Pubmed]
  16. Assessment of induction of cytochrome P450 by NO-1886 (ibrolipim), a lipoprotein lipase-promoting agent, in primary cultures of human hepatocytes and in female rat liver. Morioka, Y., Nishimura, M., Imai, T., Suzuki, S., Harada, M., Satoh, T., Naito, S. Drug Metab. Pharmacokinet. (2006) [Pubmed]
  17. Effects of NO-1886 (Ibrolipim), a lipoprotein lipase-promoting agent, on gene induction of cytochrome P450s, carboxylesterases, and sulfotransferases in primary cultures of human hepatocytes. Nishimura, M., Imai, T., Morioka, Y., Kuribayashi, S., Kamataki, T., Naito, S. Drug Metab. Pharmacokinet. (2004) [Pubmed]
  18. NO-1886 (ibrolipim), a lipoprotein lipase activator, increases the expression of uncoupling protein 3 in skeletal muscle and suppresses fat accumulation in high-fat diet-induced obesity in rats. Kusunoki, M., Tsutsumi, K., Iwata, K., Yin, W., Nakamura, T., Ogawa, H., Nomura, T., Mizutani, K., Futenma, A., Utsumi, K., Miyata, T. Metab. Clin. Exp. (2005) [Pubmed]
  19. Pharmacokinetics and metabolism of NO-1886, a lipoprotein lipase-promoting agent, in cynomolgus monkey. Morioka, Y., Harada, M., Imai, T., Naito, S. Xenobiotica (2003) [Pubmed]
  20. NO-1886 (ibrolipim), a lipoprotein lipase-promoting agent, accelerates the expression of UCP3 messenger RNA and ameliorates obesity in ovariectomized rats. Kano, S., Doi, M. Metab. Clin. Exp. (2006) [Pubmed]
  21. The novel compound NO-1886 activates lipoprotein lipase in primary cultured adipose and skeletal muscle cells. Hagi, A., Hirai, I., Kohri, H., Tsutsumi, K. Biol. Pharm. Bull. (1997) [Pubmed]
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