Lapaquistat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型有效、竞争性、口服活性角鲨烯合酶抑制剂，IC50 为 78 nM。

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.

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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.

TAK475 | TAK 475 | Lapaquistat acetate

Others

Other Targets

Other Targets

Cardiovascular Disease

Dyslipidemia

189060-13-7

645.146

C33H41ClN2O9

>98% (HPLC)

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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

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

(-20℃)

With Ice Pack

≥ 2 years