Lapaquistat

CAS No. 189060-13-7

Lapaquistat( TAK475 | TAK 475 | Lapaquistat acetate )

Catalog No. M12962 CAS No. 189060-13-7

A novel potent, competitive, orally active squalene synthase inhibitor with IC50 of 78 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 299 Get Quote
50MG 1143 Get Quote
100MG 1737 Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    Lapaquistat
  • Note
    Research use only, not for human use.
  • Brief Description
    A novel potent, competitive, orally active squalene synthase inhibitor with IC50 of 78 nM.
  • Description
    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.Dyslipidemia Phase 3 Discontinued.
  • In Vitro
    ——
  • In Vivo
    Animal Model:Male WHHLMI rabbits, aged 2 months Dosage:100 or 200?mg/kg Administration:Diet supplemented; 100 or 200?mg/kg; 32 weeks Result:Increased collagen concentration and transformed coronary plaques into fibromuscular plaques.Suppressed the expression of MMP-1 and PAI-1 in the plaque and increased peripheral coenzyme Q10 levels.
  • Synonyms
    TAK475 | TAK 475 | Lapaquistat acetate
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Other Targets
  • Research Area
    Cardiovascular Disease
  • Indication
    Dyslipidemia

Chemical Information

  • CAS Number
    189060-13-7
  • Formula Weight
    645.146
  • Molecular Formula
    C33H41ClN2O9
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C(O)CC1CCN(C(C[C@H]2O[C@H](C3=CC=CC(OC)=C3OC)C4=CC(Cl)=CC=C4N(CC(C)(C)COC(C)=O)C2=O)=O)CC1
  • 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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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