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
- Molecular Weight:
- 645.14
- MDL Number:
- MOL File:
- 189060-13-7.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| 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) |
| pka | 4.66±0.10(Predicted) |
| form | Solid |
| color | White |
| InChIKey | CMLUGNQVANVZHY-POURPWNDSA-N |
| SMILES | O=C1[C@@H](CC(N2CCC(CC(O)=O)CC2)=O)O[C@H](C3=CC=CC(OC)=C3OC)C4=C(C=CC(Cl)=C4)N1CC(C)(C)COC(C)=O |
| FDA UNII | IUH3AY74O3 |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
LAPAQUISTAT price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML2168 | TAK-475 ≥98% (HPLC) | 189060-13-7 | 5mg | $170 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML2168 | TAK-475 ≥98% (HPLC) | 189060-13-7 | 25mg | $664 | 2026-04-30 | Buy |
| TRC | TRC-L175500-25MG | Lapaquistat Acetate | 189060-13-7 | 25mg | $14585 | 2026-06-03 | Buy |
| TRC | TRC-L175500-10MG | Lapaquistat Acetate | 189060-13-7 | 10mg | $7207 | 2026-06-03 | Buy |
| Biosynth | PHA06013 | Lapaquistat acetate | 189060-13-7 | 5mg | $584.7 | 2026-06-04 | Buy |
LAPAQUISTAT Chemical Properties, Uses, 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 200mg/kg |
| Administration: | Diet supplemented; 100 or 200mg/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
LAPAQUISTAT Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| J & K SCIENTIFIC LTD. | 18210857532 18210857532 | jkinfo@jkchemical.com | China | 96815 | 76 |
| ZHIWE CHEMTECH CO LTD | 021-20221225 13917446399 | zwchem@163.com | China | 524 | 61 |
| LGM Pharma | 1-(800)-881-8210 | inquiries@lgmpharma.com | United States | 2110 | 70 |
| Chemsky (shanghai) International Co.,Ltd | 021-50135380 | shchemsky@sina.com | China | 15350 | 60 |
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| Shanghai Aladdin Bio-Chem Technology Co.,LTD | 400-6206333 13167063860 | anhua.mao@aladdin-e.com | China | 29977 | 65 |
| Wulechem Co., Ltd. | 13761914825 | wulesian@wulechem.com | China | 285 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4859 | 55 | |
| SPIRO PHARMA | eric_feng1954@126.com | China | 9239 | 55 | |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
