Uses
YM-53601 free base, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo[1]. YM-53601 free base inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent[2]. YM-53601 free base is also an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation[3].
References
[1] T Ugawa,et al. YM-53601, a novel squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in several animal species. Br J Pharmacol.2000 Sep;131(1):63-70. DOI:
10.1038/sj.bjp.0703545[2] Tsukasa Ishihara, et al. Syntheses of 3-ethylidenequinuclidine derivatives as squalene synthase inhibitors. Part 2: enzyme inhibition and effects on plasma lipid levels. Bioorg Med Chem.2003 Aug 15;11(17):3735-45. DOI:
10.1016/s0968-0896(03)00336-5[3] Eun-Mee Park,et al. Farnesyl-diphosphate farnesyltransferase 1 regulates hepatitis C virus propagation. FEBS Lett.2014 May 2;588(9):1813-20. DOI:
10.1016/j.febslet.2014.03.043[4] Joan Montero,et al.Mitochondrial cholesterol contributes to chemotherapy resistance in hepatocellular carcinoma. Cancer Res.2008 Jul 1;68(13):5246-56. DOI:
10.1158/0008-5472.CAN-07-6161
