| Identification | Back Directory | [Name]
LAPAQUISTAT | [CAS]
189060-13-7 | [Synonyms]
TAK-475
CS-1400
LAPAQUISTAT
Lapaquistat Acetate
Lapaquistat Acetate (TAK-475)
Lapaquistat and Lapaquistat Acetate
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
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
4-Piperidineacetic acid, 1-[2-[(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]- | [Molecular Formula]
C33H41ClN2O9 | [MOL File]
189060-13-7.mol | [Molecular Weight]
645.14 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
A novel squalene synthase inhibitor | [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. |
| [storage]
Store at -20°C |
|
| Company Name: |
LGM Pharma
|
| Tel: |
1-(800)-881-8210 |
| Website: |
www.lgmpharma.com |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
|