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

American Custom Chemicals Corporation

Product number: API0007318
Product name: LAPAQUISTAT ACETATE
Purity: 95.00%
Packaging: 25MG
Price: $12370.05
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

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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

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Heterocycles

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Pharmaceuticals