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Atorvastatin Calcium

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(chǎn)生。Atorvastatin Calcium 可誘導(dǎo)凋亡和自噬。

Atorvastatin Calcium  Chemical Structure

Atorvastatin Calcium Chemical Structure

CAS: 134523-03-8

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買(mǎi)數(shù)量
10mM (1mL in DMSO) 1154.03 現(xiàn)貨
50mg 897.38 現(xiàn)貨
500mg 6304.02 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Atorvastatin Calcium 相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類(lèi)型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)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(chǎn)生。Atorvastatin Calcium 可誘導(dǎo)凋亡和自噬。
靶點(diǎn)
HMG-CoA reductase [1]
(Cell-free assay)
體外研究(In Vitro)
體外研究活性

Atorvastatin以濃度和時(shí)間依賴的方式抑制pre-proET-1 mRNA表達(dá)(60-70%最大抑制),并減少免疫反應(yīng)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(xì)胞中,Atorvastatin顯著降低了血管緊張素II誘導(dǎo)和表皮生長(zhǎng)因子誘導(dǎo)的ROS產(chǎn)生。在血管平滑肌細(xì)胞中,Atorvastatin下調(diào)NAD(P)H氧化酶亞基NOX1的mRNA的表達(dá),而p22phox的mRNA的表達(dá)沒(méi)有顯著改變。Atorvastatin抑制RAC1 GTP酶的膜轉(zhuǎn)位,這需要NAD(P)H氧化酶的激活。[2]

在單核細(xì)胞和血管平滑肌細(xì)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(dǎo)的NF-κB活化。在血管緊張素Ⅱ刺激的細(xì)胞中,Atorvastatin(1 μM)減弱血管緊張素Ⅱ和腫瘤壞死因子-α誘導(dǎo)的MCP-1的表達(dá),被Mevalonate逆轉(zhuǎn)。在血管平滑肌細(xì)胞中,Atorvastatin(1 μM)減少血管緊張素Ⅱ和腫瘤壞死因子-α誘導(dǎo)的IP-10的表達(dá),并且這種降低是通過(guò)甲羥戊酸部分逆轉(zhuǎn)。[3]

Atorvastatin和Gemfibrozil的代謝產(chǎn)物,而不是母體藥物,是抗脂蛋白氧化的抗氧化劑。 [4]

實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Growth inhibition assay Cell viability 25874930
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

在statin處理過(guò)的大鼠中,Atorvastatin降低p22phox和NOX1血管mRNA的表達(dá),提高主動(dòng)脈過(guò)氧化氫酶的表達(dá)。[2]

在膽固醇喂養(yǎng)的兔子中,Atorvastatin抑制人C反應(yīng)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(dá)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

化學(xué)信息&溶解度

分子量 1155.34 分子式

2(C33H34FN2O5).Ca

CAS號(hào) 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(chǔ)存條件(自收到貨起)

體外溶解度
批次:

DMSO : 100 mg/mL ( (86.55 mM) ;DMSO吸濕會(huì)降低化合物溶解度,請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次:

現(xiàn)配現(xiàn)用,請(qǐng)按從左到右的順序依次添加,澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器(澄清溶液)

第一步:請(qǐng)輸入基本實(shí)驗(yàn)信息(考慮到實(shí)驗(yàn)過(guò)程中的損耗,建議多配一只動(dòng)物的藥量)

mg/kg g μL

第二步:請(qǐng)輸入動(dòng)物體內(nèi)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)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,:如該濃度超過(guò)該批次藥物DMSO溶解度,請(qǐng)先聯(lián)系Selleck);

體內(nèi)配方配制方法: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(nèi)配方配制方法: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(jìn)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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