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CAS No.: 134523-03-8

阿托伐他汀钙 Catalog No. CSN12530

Synonyms: CI-981;Atorvastatin hemicalcium;Atorvastatin Calcium

Atorvastatin Hemicalcium is a potent HMG-CoA reductase inhibitor with IC50 value of 8 nM.

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靶点选择性

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实验方案

技术信息

生物活性

描述Atorvastatin is an inhibitor of the enzyme 3-hydroxyl-3-methylglutaryl coenzyme A reductase used to prevent coronary heart disease,it has the ability to effectively decrease blood lipids^[5].Atorvastatin hemicalcium salt inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.^[6]. Severe liver injury occurred in diabetic rats treated with 20mg/kg atorvastatin,it also increased the secretion of pro-inflammatory factors such as L-1, TNF, IL-6, and IL-18 by enhancing activation of the NF-B signal pathway in the livers of diabetic rats. Atorvastatin elevated the levels of ROS and reduced the antioxidant enzyme (SOD and CAT) activities. Atorvastatin also increased the expression of antiapoptotic protein BCL2 and decreased the expression of pro-apoptotic protein BAX in the livers of diabetic rats^[7].Atorvastatin (20-30 mg/kg; oral gavage; once a day; for 28 days, Apolipoprotein E–deficient mice) treatment significantly reduces endoplasmic reticulum (ER) stress signaling proteins, the number of apoptotic cells, and the activation of Caspase12 and Bax in mice. Proinflammatory cytokines such as IL-6, IL-8, IL-1β are all remarkably inhibited after Atorvastatin treatment^[8].
作用机制By down-regulating GRP78, caspase-12 and CHOP expressions in myocardial cells in rat heart failure after myocardial infarction, atorvastatin treatment decreased the apoptosis of myocardial cells, by which atorvastatin functions in protecting against heart failure^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human Caco2 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay, IC50=18.7 μM	22533316
human HCEC cells	-	Cytotoxic assay	72 h	Cytotoxicity against human HCEC cells assessed as reduction in cell survival after 72 hrs by MTT assay, IC50=20.3 μM	22533316
human HeLa cells	-	Cytotoxic assay	72 h	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=4.22 μM	22533316

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动物研究
剂量
Rats: 10 mg/kg, max = 20 mg/kg^[3]

给药途径
p.o.

毒性数据 (半致死量)
Rats: 40 mg/kg p.o.^[3]
参考文献

动物研究
剂量	Rats: 10 mg/kg, max = 20 mg/kg^[3]
给药途径	p.o.
毒性数据 (半致死量)	Rats: 40 mg/kg p.o.^[3]

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
- 0.8655 mL
- 4.3277 mL
- 8.6555 mL
- 5 mM
- 0.1731 mL
- 0.8655 mL
- 1.7311 mL
- 10 mM
- 0.0866 mL
- 0.4328 mL
- 0.8655 mL

技术信息

CAS号

134523-03-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C66H68CaF2N4O10

运输

蓝冰

分子量

1155.34

别名

CI-981;Atorvastatin hemicalcium;Atorvastatin Calcium;阿托伐他汀钙

溶解度

DMSO	460.0 mg/mL (398.2 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	8 mg/mL	clear
PO	0.5% CMC-Na	60 mg/mL	suspension

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