Lapaquistat|189059-71-0|(T-91485)-陌孚医药/Medlife

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Lapaquistat (Synonyms: T-91485)

目录号: PL04306 纯度: ≥99%

CAS No. :189059-71-0

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PL04306-50mg	50mg	询价	询价
PL04306-100mg	100mg	询价	询价

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中文名称	Lapaquistat
英文名称	Lapaquistat
英文别名	4-Piperidineacetic acid, 1-[2-[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-4,1-benzoxazepin-3-yl]acetyl]-;4-Piperidineacetic acid, 1-[[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-4,1-benzoxazepin-3-yl]acetyl]- (9CI);4-Piperidineacetic acid, 1-[[7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-4,1-benzoxazepin-3-yl]acetyl]-, (3R-trans)-;T 91485;2-[1-[2-[(3R)-7-chloro-5-(2,3-dimethoxyphenyl)-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-5H-4,1-benzoxazepin-3-yl]acetyl]piperidin-4-yl]acetic acid;LAPAQUISTAT;2-(1-(2-((3R,5S)-1-(3-hydroxy-2,2-dimethylpropyl)-7-chloro-5-(2,3- dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydrobe;4-Piperidineacetic acid, 1-(((3R,5S)-1-(3-(hydroxy)-2,2-dimethylpropyl)-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-2-oxo-4,1-benzoxazepin-3-yl)acetyl)-;N-[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-acetyl]piperidine-4-acetic acid;HDGUKVZPMPJBFK-LEAFIULHSA-N;PEZ79BV72X;2-(1-(2-((3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-1,2,3,5-tetrahydrobenzo[e][1,4]oxazepin-3-yl)acetyl)piperidin-4-yl)acetic acid;4-Piperidineacetic acid,1-[[(3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1,2,3,5-tetrahydro-1-(3-hydroxy-2,2-dimethylpropyl)-2-oxo-4,1-benzoxazepin-3-yl]acetyl]-;Lapaquistat [INN];AMY24163;BDBM50118898;2-(1-(2-((3R,5S)-1-(3-hydroxy-2,2-dimethylpropy
Cas No.	189059-71-0
分子式	C₃₁H₃₉ClN₂O₈
分子量	603.10
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Lapaquistat (T-91485) 是一种胆固醇生物合成 cholesterol biosynthesis 的抑制剂，是 Lapaquistat acetate (HY-16274) 的活性代谢产物。Lapaquistat 可以降低他汀类药物在降脂中的肌毒性。

生物活性

Lapaquistat (T-91485), a cholesterol biosynthesis inhibitor, is the active metabolite of Lapaquistat acetate (HY-16274). Lapaquistat can decrease statin-induced myotoxicity in lipid-lowering therapy.

性状

Solid

IC50 & Target[1][2]

Cholesterol biosynthesis

体外研究(In Vitro)

Lapaquistat inhibits cholesterol biosynthesis in differentiated RD (rhabdomyosarcoma) cells, with an IC50 of 36 nM.
Lapaquistat potently inhibits cholesterol synthesis in RD cells, with an IC25 exceeded 100 μM.
Lapaquistat concentration-dependently inhibits cholesterol biosynthesis in human skeletal myocytes, with an IC50 of 45 nM. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

After oral administration to rats, Lapaquistat acetate (HY-16274) is absorbed and rapidly hydrolyzed into a pharmacological active metabolite, Lapaquistat. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Nishimoto T, et al. Comparing myotoxic effects of squalene synthase inhibitor, T-91485, and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors in human myocytes. Biochem Pharmacol. 2003 Dec 1;66(11):2133-9.

溶解度数据	In Vitro: DMSO : 25 mg/mL (41.45 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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