Atorvastatin
中文名称：阿托伐他汀
Atorvastatin 是一种降脂剂。 它是 hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase 的竞争性抑制剂，它可通过甲羟戊酸途径生物合成胆固醇的速率决定酶并激活自噬。
Atorvastatin Chemical Structure
CAS: 134523-00-5
客户使用Selleck的发表文献23篇
产品质控
Atorvastatin相关产品
| 相关产品 | Mevastatin SR-12813 Clinofibrate | 点击展开 |
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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
HMG-CoA Reductase抑制剂选择性比较
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 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Atorvastatin 是一种降脂剂。 它是 hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase 的竞争性抑制剂，它可通过甲羟戊酸途径生物合成胆固醇的速率决定酶并激活自噬。 |
|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04915183 | Not yet recruiting | Hearing Loss|Head and Neck Cancer |
National Institute on Deafness and Other Communication Disorders (NIDCD)|National Institutes of Health Clinical Center (CC) |
January 12 2024 | Phase 3 |
| NCT06191991 | Active not recruiting | Healthy Volunteers |
Aligos Therapeutics |
November 3 2023 | Phase 1 |
化学信息&溶解度
| 分子量 | 558.64 | 分子式 | C33H35FN2O5 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | 3年 -20°C 粉状 | ||
|
体外溶解度 |
DMSO : 100 mg/mL ( (179.0 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 17 mg/mL (30.43 mM) Water : Insoluble |
摩尔浓度计算器 |
|
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）
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）
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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