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Chemical Structure : Lapaquistat
Catalog No.: PC-61039Not For Human Use, Lab Use Only.
Lapaquistat (TAK-475) is a novel potent, competitive, orally active squalene synthase inhibitor with IC50 of 78 nM.
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Lapaquistat (TAK-475) is a novel potent, competitive, orally active squalene synthase inhibitor with IC50 of 78 nM.
Lapaquistat (TAK-475) displays no effect on plasma aspartate aminotransferase and alanine aminotransferase activities.
Lapaquistat (TAK-475) effectively inhibits cholesterol synthesis in rat liver with ED50 of 2.9 mg/kg (p.o.), lowers plasma total cholesterol, triglyceride and phospholipid levels in rabbits, also inhibits the secretion of cholesterol, triglyceride and phospholipid components of very-low-density lipoprotein (VLDL) from liver.
| M.Wt | 645.146 | |
| Formula | C33H41ClN2O9 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Miki T, et al. J Med Chem. 2002 Sep 26;45(20):4571-80.
2. Amano Y, et al. Eur J Pharmacol. 2003 Apr 11;466(1-2):155-61.
3. Nishimoto T, et al. Br J Pharmacol. 2003 Jul;139(5):911-8.
4. Burnett JR. Curr Opin Investig Drugs. 2006 Sep;7(9):850-6.
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