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LAPAQUISTAT

Product Name
LAPAQUISTAT
CAS No.
189060-13-7
Chemical Name
LAPAQUISTAT
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]-;2-(1-(2-((3R,5S)-1-(3-Acetoxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepin-3-yl)acetyl)piperidin-4-yl)acetic acid
CBNumber
CB01509119
Molecular Formula
C33H41ClN2O9
Formula Weight
645.14
MOL File
189060-13-7.mol
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LAPAQUISTAT Property

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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2168
Product name
TAK-475
Purity
≥98% (HPLC)
Packaging
5mg
Price
$150.73
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2168
Product name
TAK-475
Purity
≥98% (HPLC)
Packaging
25mg
Price
$434
Updated
2025/07/31
TRC
Product number
L175500
Product name
LapaquistatAcetate
Packaging
25mg
Price
$10725
Updated
2021/12/16
ChemScene
Product number
CS-0006278
Product name
Lapaquistatacetate
Purity
>99.0%
Packaging
1mg
Price
$160
Updated
2021/12/16
ChemScene
Product number
CS-0006278
Product name
Lapaquistatacetate
Purity
>99.0%
Packaging
5mg
Price
$480
Updated
2021/12/16
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LAPAQUISTAT Chemical Properties,Usage,Production

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.

LAPAQUISTAT Preparation Products And Raw materials

Raw materials

Preparation Products

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LAPAQUISTAT Suppliers

Canada 1 China 30 United States 7 Global 38
LGM Pharma
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1-(800)-881-8210
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615-250-9817
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inquiries@lgmpharma.com
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United States
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1-516-927-0118
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TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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marketing@targetmol.com
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United States
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Cckinase, Inc.
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+1 (732)236-3202
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sales@cckinase.com
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United States
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BOC Sciences
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16314854226
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United States
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MedChemExpress
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NE Scientific
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189060-13-7, LAPAQUISTATRelated Search:

N-Methyl 4-chloro-2-(methoxymethyl)aniline 4-PIPERIDINEACETIC ACID HYDROCHLORIDE LAPAQUISTAT 2-amino-5-chloro-diphenyl methanol

  • 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)
  • 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]-
  • 2-(1-(2-((3R,5S)-1-(3-Acetoxy-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepin-3-yl)acetyl)piperidin-4-yl)acetic acid
  • 189060-13-7
  • C33H41ClN2O9
  • Amines
  • Chiral Reagents
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals