中文名稱:阿托伐他汀
Atorvastatin 是一種降脂劑。 它是 hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase 的競爭性抑制劑,它可通過甲羥戊酸途徑生物合成膽固醇的速率決定酶并激活自噬。
Atorvastatin Chemical Structure
CAS: 134523-00-5
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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hepatocytes | Function assay | 0.1 to 10 uM | up to 90 mins | Drug metabolism in Sprague-Dawley rat hepatocytes assessed per 10'6 cells at 0.1 to 10 uM up to 90 mins by media-loss method, Km=0.43μM | 22593038 |
hepatocytes | Function assay | 0.1 to 10 uM | up to 90 mins | Drug metabolism in Sprague-Dawley rat hepatocytes assessed per 10'6 cells at 0.1 to 10 uM up to 90 mins by conventional assay, Km=1.3μM | 22593038 |
Hep3G | Function assay | 25 uM | 48 hrs | Inhibition of HMG CoA reductase in human Hep3G cells assessed as increase in LDL receptor expression at 25 uM incubated for 48 hrs by immunofluorescence method | 31005367 |
C2C12 | Function assay | 1 uM | Induction of cell differentiation in mouse C2C12 cells assessed as myosin heavy chain expression at 1 uM | 20081855 | |
HepG2 | Function assay | 1 uM | Upregulation of LDL receptor expression in human HepG2 cells at 1 uM in presence of ARH-specific siRNA | 20356098 | |
HepG2 | Function assay | 10 uM | Induction of SREBP2 maturation in human HepG2 cells at 10 uM after overnight incubation by immunoblot analysis | 26784936 | |
A549 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=8.7μM | 23570542 | |
HS68 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HS68 cells after 72 hrs by MTT assay, IC50=22.7μM | 23570542 | |
MEF | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay, IC50=30.7μM | 23570542 | |
human red blood cells | Antiplasmodial assay | 48 hrs | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells after 48 hrs by SYBR test, IC50=10.3μM | 26988303 | |
HEK293 | Function assay | TP_TRANSPORTER: uptake in OATP1B1-expressing HEK293 cells, Km=12.4μM | 15970799 | ||
L6 | Function assay | Inhibition of cholesterol synthesis in rat L6 cells assessed as incorporation of [14C]acetate into cholesterol, IC50=0.078μM | 18412317 | ||
HEK293 | Function assay | Activity at human liver OATP1B3 expressed in HEK293 Flp-In cells, Km=0.73μM | 22541068 | ||
HEK293 | Function assay | Activity at human liver OATP1B1 expressed in HEK293 Flp-In cells, Km=0.77μM | 22541068 | ||
HEK293 | Function assay | Activity at human liver OATP2B1 expressed in HEK293 Flp-In cells, Km=2.84μM | 22541068 | ||
HEK293 | Function assay | Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate, IC50=0.6μM | 22587986 | ||
HEK293 | Function assay | Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate, IC50=0.8μM | 22587986 | ||
HEK293 | Function assay | Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate, IC50=1.6μM | 22587986 | ||
A549 | Function assay | Reductase Activity Assay: The HMGR activity was performed using HMG-CoA reductase assay kit from Sigma-Aldrich with the human recombinant protein or 100 μg total cell lysates from A549 cells. Lovastatin was used as a positive control, and SAHA as a negati, IC50=0.0116μM | ChEMBL | ||
點擊查看更多細胞系數據 |
產品描述 | Atorvastatin 是一種降脂劑。 它是 hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase 的競爭性抑制劑,它可通過甲羥戊酸途徑生物合成膽固醇的速率決定酶并激活自噬。 |
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分子量 | 558.64 | 分子式 | C33H35FN2O5 |
CAS號 | 134523-00-5 | 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 | ||
儲存條件(自收到貨起) | 3年 -20°C 粉狀 | ||
體外溶解度 |
DMSO : 100 mg/mL ( (179.0 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Ethanol : 17 mg/mL (30.43 mM) Water : Insoluble |
摩爾濃度計算器 |
體內溶解度 現配現用,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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