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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
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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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