Atorvastatin Calcium
中文名称：阿托伐他汀钙
Atorvastatin Calcium 是一种 HMG-CoA reductase 抑制剂，用作降胆固醇药物，并阻断胆固醇的产生。Atorvastatin Calcium 可诱导凋亡和自噬。
Atorvastatin Calcium Chemical Structure
CAS: 134523-03-8
产品质控
批次：
纯度：
99.98%
99.98
Atorvastatin Calcium 相关产品
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|---|---|---|
| 相关化合物库 | 代谢化合物库 抗癌代谢化合物库 谷氨酰胺代谢化合物库 糖代谢化合物库 脂代谢化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| LN18 | Function assay | 1 to 3 uM | 24 hrs | Inhibition of DNA synthesis in human LN18 cells assessed as inhibition of tritiated thymidine incorporation at 1 to 3 uM after 24 hrs by beta counting | 22533316 |
| LN229 | Function assay | 1 to 3 uM | 24 hrs | Inhibition of DNA synthesis in human LN229 cells assessed as inhibition of tritiated thymidine incorporation at 1 to 3 uM after 24 hrs by beta counting | 22533316 |
| KB | Cytotoxicity assay | 72 hrs | Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=1.97μM. | 22533316 | |
| Me300 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Me300 cells after 72 hrs by MTT assay, IC50=1.2μM. | 22533316 | |
| HeLa | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=4.22μM. | 22533316 | |
| LN18 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human LN18 cells assessed as reduction in cell survival after 72 hrs by MTT assay, IC50=6.9μM. | 22533316 | |
| LNZ308 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human LNZ308 cells after 72 hrs by MTT assay, IC50=7.44μM. | 22533316 | |
| LN229 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human LN229 cells assessed as reduction in cell survival after 72 hrs by MTT assay, IC50=8.1μM. | 22533316 | |
| Caco2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay, IC50=18.7μM. | 22533316 | |
| HCEC | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCEC cells assessed as reduction in cell survival after 72 hrs by MTT assay, IC50=20.3μM. | 22533316 | |
| CHO | Function assay | pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells, IC50=3.38844μM. | 23571415 | ||
| CHO | Function assay | Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells, Ki=2.58μM. | 23571415 | ||
| CHO | Function assay | pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells, IC50=0.81283μM. | 23571415 | ||
| CHO | Function assay | Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells, Ki=0.45μM. | 23571415 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Atorvastatin Calcium 是一种 HMG-CoA reductase 抑制剂，用作降胆固醇药物，并阻断胆固醇的产生。Atorvastatin Calcium 可诱导凋亡和自噬。 | |
|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Atorvastatin以浓度和时间依赖的方式抑制pre-proET-1 mRNA表达（60-70％最大抑制），并减少免疫反应ET-1的水平（25-50％），在氧化的低密度脂蛋白（1-50毫克/毫升）存在下保持这种抑制效果。[1] 在血管平滑肌细胞中，Atorvastatin显著降低了血管紧张素II诱导和表皮生长因子诱导的ROS产生。在血管平滑肌细胞中，Atorvastatin下调NAD（P）H氧化酶亚基NOX1的mRNA的表达，而p22phox的mRNA的表达没有显著改变。Atorvastatin抑制RAC1 GTP酶的膜转位，这需要NAD（P）H氧化酶的激活。[2] 在单核细胞和血管平滑肌细胞中，Atorvastatin（0.1 μM）显著减少血管紧张素Ⅱ和肿瘤坏死因子-α诱导的NF-κB活化。在血管紧张素Ⅱ刺激的细胞中，Atorvastatin（1 μM）减弱血管紧张素Ⅱ和肿瘤坏死因子-α诱导的MCP-1的表达，被Mevalonate逆转。在血管平滑肌细胞中，Atorvastatin（1 μM）减少血管紧张素Ⅱ和肿瘤坏死因子-α诱导的IP-10的表达，并且这种降低是通过甲羟戊酸部分逆转。[3] Atorvastatin和Gemfibrozil的代谢产物，而不是母体药物，是抗脂蛋白氧化的抗氧化剂。 [4] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Growth inhibition assay | Cell viability |
|
25874930 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在statin处理过的大鼠中，Atorvastatin降低p22phox和NOX1血管mRNA的表达，提高主动脉过氧化氢酶的表达。[2] 在胆固醇喂养的兔子中，Atorvastatin抑制人C反应蛋白的血清水平的增加。在高胆固醇血症的瓣叶，Atorvastatin抑制骨桥蛋白的表达的增加。[5] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01555632 | Withdrawn | Recurrent Prostate Cancer|Stage I Prostate Cancer|Stage IIA Prostate Cancer|Stage IIB Prostate Cancer|Stage III Prostate Cancer|Stage IV Prostate Cancer |
University of Nebraska|National Cancer Institute (NCI) |
March 2012 | Not Applicable |
化学信息&溶解度
| 分子量 | 1155.34 | 分子式 | 2(C33H34FN2O5).Ca |
| CAS号 | 134523-03-8 | SDF | Download Atorvastatin Calcium SDF |
| Smiles | CC(C)C1=C(C(=C(N1CCC(CC(CC(=O)[O-])O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4.CC(C)C1=C(C(=C(N1CCC(CC(CC(=O)[O-])O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4.[Ca+2] | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (86.55 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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