Atorvastatin Calcium (CI-981)

目錄號(hào)：S2077 Purity: 99.98%

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 (CI-981) Chemical Structure

CAS: 134523-03-8

規(guī)格	價(jià)格	庫存
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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產(chǎn)品質(zhì)控

批次：純度： 99.98%

99.98

Atorvastatin Calcium (CI-981)相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	Mevastatin Clinofibrate SR-12813	點(diǎn)擊展開
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細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息(PMID)
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
實(shí)驗(yàn)圖片	Growth inhibition assay	Cell viability		25874930

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在statin處理過的大鼠中，Atorvastatin降低p22phox和NOX1血管mRNA的表達(dá)，提高主動(dòng)脈過氧化氫酶的表達(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]

體內(nèi)研究(In Vivo)

體內(nèi)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(dá)，提高主動(dòng)脈過氧化氫酶的表達(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
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻(xiàn)
https://pubmed.ncbi.nlm.nih.gov/9637705/ https://pubmed.ncbi.nlm.nih.gov/17369473/ https://pubmed.ncbi.nlm.nih.gov/10559511/ https://pubmed.ncbi.nlm.nih.gov/9690910/ https://pubmed.ncbi.nlm.nih.gov/12045173/ + 展開

參考文獻(xiàn)

https://pubmed.ncbi.nlm.nih.gov/9637705/
https://pubmed.ncbi.nlm.nih.gov/17369473/
https://pubmed.ncbi.nlm.nih.gov/10559511/

https://pubmed.ncbi.nlm.nih.gov/9690910/
https://pubmed.ncbi.nlm.nih.gov/12045173/

+ 展開