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中文名稱:阿托伐他汀鈣
Atorvastatin Calcium 是一種 HMG-CoA reductase 抑制劑,用作降膽固醇藥物,并阻斷膽固醇的產生。Atorvastatin Calcium 可誘導凋亡和自噬。
Atorvastatin Calcium Chemical Structure
CAS: 134523-03-8
相關產品 | Mevastatin SR-12813 Clinofibrate | 點擊展開 |
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相關化合物庫 | 代謝化合物庫 抗癌代謝化合物庫 谷氨酰胺代謝化合物庫 糖代謝化合物庫 脂代謝化合物庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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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 | ||
點擊查看更多細胞系數(shù)據(jù) |
產品描述 | Atorvastatin Calcium 是一種 HMG-CoA reductase 抑制劑,用作降膽固醇藥物,并阻斷膽固醇的產生。Atorvastatin Calcium 可誘導凋亡和自噬。 | |
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Atorvastatin以濃度和時間依賴的方式抑制pre-proET-1 mRNA表達(60-70%最大抑制),并減少免疫反應ET-1的水平(25-50%),在氧化的低密度脂蛋白(1-50毫克/毫升)存在下保持這種抑制效果。[1] 在血管平滑肌細胞中,Atorvastatin顯著降低了血管緊張素II誘導和表皮生長因子誘導的ROS產生。在血管平滑肌細胞中,Atorvastatin下調NAD(P)H氧化酶亞基NOX1的mRNA的表達,而p22phox的mRNA的表達沒有顯著改變。Atorvastatin抑制RAC1 GTP酶的膜轉位,這需要NAD(P)H氧化酶的激活。[2] 在單核細胞和血管平滑肌細胞中,Atorvastatin(0.1 μM)顯著減少血管緊張素Ⅱ和腫瘤壞死因子-α誘導的NF-κB活化。在血管緊張素Ⅱ刺激的細胞中,Atorvastatin(1 μM)減弱血管緊張素Ⅱ和腫瘤壞死因子-α誘導的MCP-1的表達,被Mevalonate逆轉。在血管平滑肌細胞中,Atorvastatin(1 μM)減少血管緊張素Ⅱ和腫瘤壞死因子-α誘導的IP-10的表達,并且這種降低是通過甲羥戊酸部分逆轉。[3] Atorvastatin和Gemfibrozil的代謝產物,而不是母體藥物,是抗脂蛋白氧化的抗氧化劑。 [4] |
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實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
Growth inhibition assay | Cell viability |
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25874930 |
體內研究(In Vivo) | ||
體內研究活性 | 在statin處理過的大鼠中,Atorvastatin降低p22phox和NOX1血管mRNA的表達,提高主動脈過氧化氫酶的表達。[2] 在膽固醇喂養(yǎng)的兔子中,Atorvastatin抑制人C反應蛋白的血清水平的增加。在高膽固醇血癥的瓣葉,Atorvastatin抑制骨橋蛋白的表達的增加。[5] |
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NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
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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 |
分子量 | 1155.34 | 分子式 | 2(C33H34FN2O5).Ca |
CAS號 | 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] | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 100 mg/mL ( (86.55 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
體內溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內配方計算器 |
動物體內配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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