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ChemicalBook--->CAS DataBase List--->189060-13-7

189060-13-7

189060-13-7 Structure

189060-13-7 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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
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