货号:A499522 同义名: CI-981;Atorvastatin hemicalcium
Atorvastatin hemicalcium salt(CI-981)是一种口服活性的3-羟基-3-甲基戊二酰辅酶A(HMG-CoA)还原酶抑制剂,有效降低血脂。它抑制人SV-SMC增殖和侵袭的IC50值分别为0.39 μM和2.39 μM。
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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 | |
human KB cells | Cytotoxic assay | 72 h | Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=1.97 μM | 22533316 | |
Dose | Rats: 10 mg/kg, max = 20 mg/kg[3] |
Administration | p.o. |
Toxicity (LD50) | Rats: 40 mg/kg p.o.[3] |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 134523-03-8 |
分子式 | C66H68CaF2N4O10 |
分子量 | 1155.342 |
别名 | CI-981;Atorvastatin hemicalcium;Atorvastatin Calcium |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,2-8°C |
溶解方案 |
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 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
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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 |