Atorvastatin (阿托伐他汀) | HMG-CoA还原酶抑制剂 | MedChemExpress (MCE)-技术前沿-资讯-生物在线

Atorvastatin (阿托伐他汀) | HMG-CoA还原酶抑制剂 | MedChemExpress (MCE)

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Atorvastatin (阿托伐他汀)

国际站:Atorvastatin

CAS:134523-00-5

纯度:96.24%

分子量:558.64

Formula:C33H35FN2O5

运输条件:Room temperature in continental US; may vary elsewhere.

储存方式:

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

产品活性:Atorvastatin 是一种具有口服活性的 HMG-CoA 还原酶抑制剂,具有有效降低血脂的能力。Atorvastatin 以 IC50 值分别为 0.39 μM 和 2.39 μM 来抑制人 SV-SMC 细胞的增殖和侵袭。

生物活性:阿托伐他汀是一种口服活性HMG-CoA还原酶抑制剂,具有有效降低血脂的能力。阿托伐他汀抑制人SV-SMC增殖和侵袭的ic50分别为0.39 μM和2.39 μM[1][2][3]。

体外:阿托伐他汀治疗通过下调心肌梗死后心肌细胞GRP78、caspase-12和CHOP的表达,减少心肌细胞凋亡,内质网(ER)应激在心衰和血管紧张素II (Ang II)刺激下被激活[4]。

体内:阿托伐他汀(20-30 mg/kg;口服填喂法;一天一次;28天;ApoE-/-小鼠)处理显著降低了Ang ii诱导的ApoE-/-小鼠内质网(ER)应激信号蛋白、凋亡细胞数量以及Caspase12和Bax的激活。促炎细胞因子如IL-6、IL-8、IL-1β在阿托伐他汀治疗后均明显受到抑制[5]。

参考文献:

[1]. Santodomingo-Garzón T, et al. Atorvastatin inhibits inflammatory hypernociception. Br J Pharmacol. 2006 Sep;149(1):14-22.

[2]. Turner NA, et al. Comparison of the efficacies of five different statins on inhibition of human saphenous vein smooth muscle cell proliferation and invasion. J Cardiovasc Pharmacol. 2007 Oct;50(4):458-61.

[3]. Nawrocki, J.W., et al., Reduction of LDL cholesterol by 25% to 60% in patients with primary hypercholesterolemia by atorvastatin, a new HMG-CoA reductase inhibitor. Arterioscler Thromb Vasc Biol, 1995. 15(5): p. 678-82. [Content Brief]

[4]. Song XJ, et al. Atorvastatin inhibits myocardial cell apoptosis in a rat model with post-myocardial infarction heart failure by downregulating ER stress response. Int J Med Sci. 2011;8(7):564-72.

[5]. Li Y, et al. Inhibition of endoplasmic reticulum stress signaling pathway: A new mechanism of statins to suppress the development of abdominal aortic aneurysm. PLoS One. 2017 Apr 3;12(4):e0174821.

[6]. Ming-Bai Hu, et al. Atorvastatin induces autophagy in MDA-MB-231 breast cancer cells. Ultrastruct Pathol. Sep-Oct 2018;42(5):409-415.

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