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Lapaquistat

Chemical Structure Lapaquistat

CAS No.: 189060-13-7

Lapaquistat(TAK475;TAK 475;Lapaquistat acetate)

Catalog No.GY05477Research Only, Not for Human Use!

Lapaquistat (TAK475

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Purity & Documentation Purity: > 98%(HPLC) Select Batch:

Biological Activity

Lapaquistat (TAK475;TAK 475;Lapaquistat acetate) is a novel potent, competitive, orally active squalene synthase inhibitor with IC50 of 78 nM; displays no effect on plasma aspartate aminotransferase and alanine aminotransferase activities; 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.

Physicochemical Properties

M.Wt 645.146
Formula C33H41ClN2O9
CAS No. 189060-13-7
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 3 Month
Shipping
Solubility

Chemical Name 1-{2-[(3R,5S)-1-(3-acetoxy-2,2-dimethylpropyl)-7-chloro-1,2,3,5-tetrahydro-2-oxo-5-(2,3-dimethoxyphenyl)-4,1-benzoxazepine-3-yl] acetyl} piperidin-4-acetic acid

Clinical Information

Dyslipidemia
Phase 3 Discontinued

References

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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