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Atorvastatin hemicalcium salt

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Chemical Structure| 134523-03-8 同义名 : CI-981;Atorvastatin hemicalcium;Atorvastatin Calcium
CAS号 : 134523-03-8
货号 : A499522
分子式 : C66H68CaF2N4O10
纯度 : 97%
分子量 : 1155.342
MDL号 : MFCD03613598
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(43.28 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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

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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.87mL

0.17mL

0.09mL

4.33mL

0.87mL

0.43mL

8.66mL

1.73mL

0.87mL
参考文献

[1]Colhoun HM, Betteridge DJ, et al. Primary prevention of cardiovascular disease with atorvastatin in type 2 diabetes in the Collaborative Atorvastatin Diabetes Study (CARDS): multicentre randomised placebo-controlled trial. Lancet. 2004;364(9435):685-96.

[2]Zhang L, He H, Balschi JA. Metformin and phenformin activate AMP-activated protein kinase in the heart by increasing cytosolic AMP concentration. Am J Physiol Heart Circ Physiol. 2007;293(1):H457-66.

[3]Crespo MJ, Quidgley J. Simvastatin, atorvastatin, and pravastatin equally improve the hemodynamic status of diabetic rats. World J Diabetes. 2015;6(10):1168-78.

[4] Song XJ, et al. Atorvastatin inhibits myocardial cell apoptosis in a rat model with post-myocardial infarction heart failure by downregulating ER stress response. Int J Med Sci. 2011;8(7):564-72.

[5] Santodomingo-Garzón T, et al. Atorvastatin inhibits inflammatory hypernociception. Br J Pharmacol. 2006 Sep;149(1):14-22.

[6] Turner NA, et al. Comparison of the efficacies of five different statins on inhibition of human saphenous vein smooth muscle cell proliferation and invasion. J Cardiovasc Pharmacol. 2007 Oct;50(4):458-61.

[7] Tianshu Chu,et al. Atorvastatin Reduces Accumulation of Vascular Smooth Muscle Cells to Inhibit Intimal Hyperplasia via p38 MAPK Pathway Inhibition in a Rat Model of Vein Graft, Arq Bras Cardiol. 2020 Oct;115(4):630-636.

[8]Li Y, et al. Inhibition of endoplasmic reticulum stress signaling pathway: A new mechanism of statins to suppress the development of abdominal aortic aneurysm. PLoS One. 2017 Apr 3;12(4):e0174821.