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首页 / 抑制剂/激动剂 / 代谢酶 / HMGCR / Atorvastatin

阿托伐他汀 /Atorvastatin {[allProObj[0].p_purity_real_show]}

货号：A430758 同义名： 阿伐他汀

Atorvastatin是一种口服活性HMG-CoA还原酶抑制剂，有效降低血脂。阿托伐他汀抑制人类SV-SMC增殖和侵袭的IC50值分别为0.39 μM和2.39 μM。

Atorvastatin 化学结构 CAS号：134523-00-5
Atorvastatin 化学结构
CAS号：134523-00-5
Atorvastatin 3D分子结构
CAS号：134523-00-5
Atorvastatin 化学结构 CAS号：134523-00-5
Atorvastatin 3D分子结构 CAS号：134523-00-5
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Atorvastatin 纯度/质量文件 产品仅供科研

货号：A430758 标准纯度： {[allProObj[0].p_purity_real_show]}
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Atorvastatin 生物活性

描述 Atorvastatin inhibits pre-proET-1 mRNA expression in a concentration- and time-dependent fashion (60-70% maximum inhibition) and reduces immunoreactive ET-1 levels (25-50%), this inhibitory effect is maintained in the presence of oxidized LDL (1-50 mg/mL). Atorvastatin significantly reduces angiotensin II-induced and epidermal growth factor-induced ROS production in VSMCs. Atorvastatin downregulates mRNA expression of the NAD(P)H oxidase subunit nox1 in VSMCs, whereas p22phox mRNA expression is not significantly altered. Atorvastatin inhibits membrane translocation of rac1 GTPase, which is required for the activation of NAD(P)H oxidase. Atorvastatin (0.1 μM) significantly diminishes NF-κB activation induced by Ang II and TNF-α in mononuclear cells and VSMC. Atorvastatin (1 μM) diminishes MCP-1 expression induced by Ang II, TNF-α and is reversed by Mevalonate only in Ang II-stimulated cells. Atorvastatin (1 μM) diminishes IP-10 expression induced by Ang II and by TNF-α in VSMC, and this reduction is partially reversed by Mevalonate. Atorvastatin and Gemfibrozil metabolites, but not the parent drugs, are potent antioxidants against lipoprotein oxidation.[1-2]

Atorvastatin 动物研究

Dose Rats: 10 mg/kg, max = 20 mg/kg[3]
Administration p.o.
Toxicity (LD50) Rats: 40 mg/kg p.o.[3]

Atorvastatin 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00768638 Chronic Kidney Disease Phase 4 Completed - Canada ... 展开 >> Hôtel-Dieu de Québec Hospital Quebec, Canada, G1R2J6 收起 <<
NCT02497638 Prostate Cancer Phase 2 Not yet recruiting December 2022 Canada, Ontario ... 展开 >> Princess Margaret Cancer Centre Recruiting Toronto, Ontario, Canada, M5G 2M9 Principal Investigator: Robert Hamilton, MD, MPH, FRCSC          Principal Investigator: Neil Fleshner, MD, MPH, FRCSC 收起 <<
NCT00974740 Type 1 Diabetes Phase 1 Terminated(for lack of recruit... 展开 >>ment) 收起 << - Germany ... 展开 >> Diabetes-Zentrum Mergentheim Bad Mergentheim, Germany, 97980 Gemeinschaftskrankenhaus Havelhöhe Berlin, Germany, 14089 Helios Klinikum Emil von Behring Berlin, Germany, 14165 Praxis Dr. Friedhelm Schmitten Bestwig-Ramsbeck, Germany, 59909 DDZ Deutsches Diabetes Zentrum Düsseldorf, Germany, 40221 St. Josefs Krankenhaus Heidelberg, Germany, 69115 St. Antonius Krankenhaus, Med. Klinik Köln, Germany, 50968 Praxisklinik Leipzig Leipzig, Germany, 04103 Praxis Dr. Gerhard Willms Leverkusen, Germany, 51373 Praxis Dr. Heinz-Georg Ley Marl, Germany, 45770 Diabetologische Schwerpunktpraxis, Angiologie Münster, Germany, 48145 Praxis Dr. Werner Stürmer Würzburg, Germany, 97070 收起 <<

Atorvastatin 参考文献

[1]Colhoun HM, Betteridge DJ, et al. Primary prevention of cardiovascular disease with atorvastatin in type 2 diabetes in the Collaborative Atorvastatin Diabetes Study (CARDS): multicentre randomised placebo-controlled trial. Lancet. 2004;364(9435):685-96.

[2]Zhang L, He H, Balschi JA. Metformin and phenformin activate AMP-activated protein kinase in the heart by increasing cytosolic AMP concentration. Am J Physiol Heart Circ Physiol. 2007;293(1):H457-66.

[3]Crespo MJ, Quidgley J. Simvastatin, atorvastatin, and pravastatin equally improve the hemodynamic status of diabetic rats. World J Diabetes. 2015;6(10):1168-78.

Atorvastatin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.79mL

0.36mL

0.18mL

8.95mL

1.79mL

0.90mL

17.90mL

3.58mL

1.79mL

Atorvastatin 技术信息

CAS号134523-00-5
分子式C33H35FN2O5
分子量 558.64
别名 阿伐他汀
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 50 mg/mL(89.5 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Atorvastatin | 阿伐他汀 | HMGCR | AmBeed-信号通路专用抑制剂 | Atorvastatin 纯度/质量文件 | Atorvastatin 生物活性 | Atorvastatin 动物研究 | Atorvastatin 临床数据 | Atorvastatin 参考文献 | Atorvastatin 实验方案 | Atorvastatin 技术信息

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