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SQS
/ Lapaquistat acetate

Lapaquistat acetate {[allProObj[0].p_purity_real_show]}

货号：A357554 同义名： TAK-475

Lapaquistat acetate是一种角鲨烯合成酶抑制剂，具有降胆固醇作用。

Lapaquistat acetate 化学结构 CAS号：189060-13-7
Lapaquistat acetate 化学结构
CAS号：189060-13-7
Lapaquistat acetate 3D分子结构
CAS号：189060-13-7
Lapaquistat acetate 化学结构 CAS号：189060-13-7
Lapaquistat acetate 3D分子结构 CAS号：189060-13-7
规格 价格 会员价 库存 数量
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Lapaquistat acetate 纯度/质量文件 产品仅供科研

货号：A357554 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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Lapaquistat acetate 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].

Lapaquistat acetate 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 - -

Lapaquistat acetate 参考文献

[1]Stein EA, Bays H, et al. Lapaquistat acetate: development of a squalene synthase inhibitor for the treatment of hypercholesterolemia. Circulation. 2011 May 10;123(18):1974-85.

[2]Shiomi M, Yamada S, et al. Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid-rich coronary plaques of hypercholesterolaemic rabbits into fibrous lesions. Br J Pharmacol. 2008 Jul;154(5):949-57.

[3]Yafeng Song,et al. Production of Squalene in Bacillus subtilis by Squalene Synthase Screening and Metabolic Engineering. J Agric Food Chem. 2020 Apr 15;68(15):4447-4455.

[4]Yi-Fang Yang,et al. Squalene synthase induces tumor necrosis factor receptor 1 enrichment in lipid rafts to promote lung cancer metastasis. Am J Respir Crit Care Med.2014 Sep 15;190(6):675-87.

[5]Stein EA, et al. Lapaquistat acetate: development of a squalene synthase inhibitor for the treatment of hypercholesterolemia. Circulation. 2011 May 10;123(18):1974-85.

[6]Marcuzzi A, et al. Repositioning of Tak-475 In Mevalonate Kinase Disease: Translating Theory Into Practice. Curr Med Chem. 2018;25(24):2783-2796.

[7]M Shiomi, et al. Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid-rich coronary plaques of hypercholesterolaemic rabbits into fibrous lesions. Br J Pharmacol. 2008 Jul;154(5):949-57.

Lapaquistat acetate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.55mL

0.31mL

0.16mL

7.75mL

1.55mL

0.78mL

15.50mL

3.10mL

1.55mL

Lapaquistat acetate 技术信息

CAS号189060-13-7
分子式C33H41ClN2O9
分子量 645.14
SMILES Code O=C(O)CC1CCN(C(C[C@H]2O[C@H](C3=CC=CC(OC)=C3OC)C4=CC(Cl)=CC=C4N(CC(C)(C)COC(C)=O)C2=O)=O)CC1
MDL No. MFCD06407873
别名 TAK-475
运输蓝冰
InChI Key CMLUGNQVANVZHY-POURPWNDSA-N
Pubchem ID 9874248
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一

Tags: Lapaquistat | 189060-13-7 | TAK-475 | TAK475 | TAK 475 | Squalene Synthase Inhibitor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lapaquistat acetate 纯度/质量文件 | Lapaquistat acetate 生物活性 | Lapaquistat acetate 临床数据 | Lapaquistat acetate 参考文献 | Lapaquistat acetate 实验方案 | Lapaquistat acetate 技术信息

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