|2-(1-(2-((3R,5S)-1-(3-乙酰氧基-2,2-二甲基丙基)-7-氯-5-(2,3-二甲氧基苯基)-2-氧代-1,2,3,5-四氢苯并[e][1,4]氧氮杂卓-3-基)乙酰基)哌啶-4-基)乙酸|CsnPharm

CAS No.: 189060-13-7

Lapaquistat acetate Catalog No. CSN20634

Synonyms: TAK-475

Lapaquistat acetate is a squalene synthase inhibitor with cholesterol-lowering effect.

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技术信息

生物活性

描述Squalene synthase (SQS) catalyzes the conversion of two farnesyl pyrophosphates to squalene, an important intermediate in between isoprene and valuable triterpenoids^[3]. Squalene synthase was up-regulated in CL1-5 cells and in the tumor regions of the lung cancer specimens. Loss of function or knockdown of SQS significantly inhibited invasion/migration and metastasis in cell and animal models and vice versa. High expression of SQS was significantly associated with poor prognosis among patients with lung cancer. Mechanistically, SQS contributed to a lipid-raft-localized enrichment of tumor necrosis factor receptor 1 in a cholesterol-dependent manner, which resulted in the enhancement of nuclear factor-κB activation leading to matrix metallopeptidase 1 up-regulation^[4]. Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway^[5]. Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research^[6]. 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^[7].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00143676	Hypercholesterolemia	Phase 3	Completed	-	-
NCT00286481	Hypercholesterolemia	Phase 3	Completed	-	-
NCT00256178	Hypercholesterolemia	Phase 3	Completed	-	-

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实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5501 mL
- 7.7503 mL
- 15.5005 mL
- 5 mM
- 0.3100 mL
- 1.5501 mL
- 3.1001 mL
- 10 mM
- 0.1550 mL
- 0.7750 mL
- 1.5501 mL

技术信息

CAS号	189060-13-7	储存条件	粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C33H41ClN2O9	运输	蓝冰
分子量	645.14	别名	TAK-475

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00143676	Hypercholesterolemia	Phase 3	Completed	-	-
NCT00286481	Hypercholesterolemia	Phase 3	Completed	-	-
NCT00256178	Hypercholesterolemia	Phase 3	Completed	-	-
NCT00249899	Hypercholesterolemia	Phase 3	Terminated(Overall profile of ... more >>the compound does not offer significant clinical advantage to patients over currently available lipid lowering agents) Collapse <<	-	-
NCT00143663	Dyslipidemia	Phase 3	Completed	-	-
NCT00865228	Hypercholesterolemia	Phase 2	Terminated(Overall profile of ... more >>the compound does not offer significant clinical advantage to patients over currently available lipid lowering agents) Collapse <<	-	United States, California ... more >> Long Beach, California, United States Sacramento, California, United States San Diego, California, United States United States, Florida Hollywood, Florida, United States Jacksonville, Florida, United States New Port Richey, Florida, United States United States, Illinois Chicago, Illinois, United States United States, Kansas Wichita, Kansas, United States United States, Kentucky Louisville, Kentucky, United States United States, New Jersey Margate, New Jersey, United States United States, North Carolina Charlotte, North Carolina, United States Raleigh, North Carolina, United States Statesville, North Carolina, United States Wilmington, North Carolina, United States Winston-Salem, North Carolina, United States United States, Oregon Medford, Oregon, United States United States, Pennsylvania Perkasie, Pennsylvania, United States Sellerville, Pennsylvania, United States United States, Tennessee Bristol, Tennessee, United States United States, Virginia Norfolk, Virginia, United States Richmond, Virginia, United States United States, Wisconsin Madison, Wisconsin, United States Collapse <<
NCT00864643	Hypercholesterolemia	Phase 2	Completed	-	-
NCT00890448	-	-	Completed	-	-
NCT00268697	Hypercholesterolemia	Phase 3	Completed	-	Estonia ... more >> Tallinn, Estonia Tartu, Estonia Latvia Riga, Latvia Russian Federation Moscow, Russian Federation Saratov, Russian Federation Smolensk, Russian Federation St. Petersburg, Russian Federation Tyumen, Russian Federation Serbia Kragujevac, Serbia Collapse <<
NCT00249912	Hypercholesterolemia	Phase 3	Completed	-	-
NCT00251680	Type 2 Diabetes	Phase 3	Completed	-	-
NCT00532311	Hypercholesterolemia	Phase 3	Terminated(Overall profile of ... more >>the compound does not offer significant clinical advantage to patients over currently available lipid lowering agents) Collapse <<	-	-
NCT00813527	Hyperlipidemias	Phase 2	Completed	-	-
NCT00487994	Dyslipidemia	Phase 3	Completed	-	-
NCT00868127	Hypercholesterolemia	Phase 3	Completed	-	-
NCT00263081	Hypercholesterolemia	Phase 3	Terminated(Overall profile of ... more >>the compound does not offer significant clinical advantage to patients over currently available lipid lowering agents) Collapse <<	-	United States, Ohio ... more >> Cincinnati, Ohio, United States Columbus, Ohio, United States Canada Québec, Canada France Paris, France Strasbourg, France Israel Jerusalem, Israel Poland Bialystok, Poland Warszawa, Poland Zabrze, Poland United Kingdom Manchester, United Kingdom Collapse <<
NCT00532558	Hypercholesterolemia	Phase 3	Terminated(Overall profile of ... more >>the compound does not offer significant clinical advantage to patients over currently available lipid lowering agents) Collapse <<	-	-

Lapaquistat acetate Catalog No. CSN20634

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