LAPAQUISTAT
LAPAQUISTAT Basic information
- Product Name:
- LAPAQUISTAT
- Synonyms:
-
- LAPAQUISTAT
- Lapaquistat and Lapaquistat Acetate
- Lapaquistat Acetate
- 2-[1-[2-[1-(3-Acetoxy-2,2-diMethylpropyl)-7-chloro-5(S)-(2,3-diMethoxyphenyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepin-3(R)-yl]acetyl]piperidin-4-yl]acetic acid
- TAK-475
- 1-[[(3R,5S)-1-[3-(Acetyloxy)-2,2-dimethylpropyl]-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-2-oxo-4,1-benzoxazepin-3-yl]acetyl]-4-piperidineacetic acid
- CS-1400
- Lapaquistat Acetate (TAK-475)
- CAS:
- 189060-13-7
- MF:
- C33H41ClN2O9
- MW:
- 645.14
- Product Categories:
-
- Amines
- Chiral Reagents
- Heterocycles
- Inhibitors
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Mol File:
- 189060-13-7.mol
LAPAQUISTAT Chemical Properties
- Melting point:
- 194-196℃
- Boiling point:
- 826.4±65.0 °C(Predicted)
- Density
- 1.246±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
- form
- Solid
- pka
- 4.66±0.10(Predicted)
- color
- White
LAPAQUISTAT Usage And Synthesis
Uses
A novel squalene synthase inhibitor. Lapaquistat acetate decreased plasma cholesterol and triglyceride levels, by lowering lipoproteins containing apoB100. Treatment with Lapaquistat acetate increased collagen concentration and transformed coronary plaques into fibromuscular plaques. Lapaquistat acetate also suppressed the expression of matrix metalloproteinase-1 and plasminogen activator inhibitor-1 in the plaque and increased peripheral coenzyme Q10 levels.Antiarteriosclerotics.
Biological Activity
TAK-475 (Lapaquist at acetate) is a potent and selective squalene synthase inhibitor. TAK-475 effectively lowers low-density lipoprotein cholesterol in human. Clinical development of TAK-475 was discontinued due to hepatotoxicity seen in two patients receiving a high dose.
in vivo
Lapaquistat acetate (diet supplemented; 100 or 200 mg/kg; 32 weeks) decreases plasma cholesterol and triglyceride levels. It delays progression of coronary atherosclerosis and changes coronary atheromatous plaques from unstable, macrophage/lipid accumulation-rich, lesions to stable fibromuscular lesions in vivo[3].
| Animal Model: | Male WHHLMI rabbits, aged 2 months[3] |
| 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. |
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