Alirocumab
MCE 国际站：Alirocumab
CAS：1245916-14-6
品牌：MedChemExpress (MCE)
存储条件：Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性：Alirocumab (REGN 727) 是一种抑制前蛋白转化酶枯草杆菌蛋白酶/kexin 9 型(PCSK9) 的人单克隆抗体。 Alirocumab 特异性结合 PCSK9，PCSK9 是肝脏低密度脂蛋白 (LDL) 受体的下调剂，从而增加肝脏结合 LDL-胆固醇 (LDL-C) 的能力并降低血液中的 LDL-C 水平。 Alirocumab可用于高胆固醇血症的研究[1][2]。
体外：Alirocumab (0.01, 0.1, 1, 2和10 μM, 24-72 h) 在 hiPSC-CMs 和 hESC-CMs 中不影响细胞活力和功能，可用于评估降脂心血管细胞中的药物安全性[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内：Alirocumab (3或10 mg/kg, 每周皮下注射持续18周) 在小鼠中可抑制动脉粥样硬化，改善斑块形态，增强他汀类药物的作用[4]。 Alirocumab (10 mg/kg, 第 0, 10, 20 天腹腔注射) 在大鼠中可通过抑制 PCSK9 改善 BDL 诱导的肝硬化大鼠的全身氧化应激和高脂血症[5]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CETP mice model[4] Dosage: 3 or 10 mg/kg Administration: s.c. Result: Decreased total cholesterol dose-dependently. Increased hepatic LDL receptor protein levels but did not affect hepatic cholesterol and TG content. Decreased atherosclerotic lesion size and improved plaque morphology. Animal Model: Rat model (240-280 g) [5] Dosage: 10 mg/kg Administration: i.p. Result: Elevated ammonia, total cholesterol, LDL and ox-LDL levels. Decreased plasma levels of total cholesterol, LDL, and oxidative stress markers. Clinical Trial
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研究领域：Metabolic Enzyme/Protease
作用靶点：Ser/Thr Protease
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参考文献：
[1]. Markham A. Alirocumab: First Global Approval. Drugs. 2015;75(14):1699-1705. [2]. Tavori H, et al. Alirocumab: PCSK9 inhibitor for LDL cholesterol reduction. Expert Rev Cardiovasc Ther. 2014 Oct;12(10):1137-44.[3]. Ni X, et al. Establishment of an in vitro safety assessment model for lipid-lowering drugs using same-origin human pluripotent stem cell-derived cardiomyocytes and endothelial cells. Acta Pharmacol Sin. 2022 Jan;43(1):240-250.[4]. Kühnast S, et al. Alirocumab inhibits atherosclerosis, improves the plaque morphology, and enhances the effects of a statin. J Lipid Res. 2014 Oct;55(10):2103-12.[5]. Huang HC, et al. Effects of PCSK-9 Inhibition by Alirocumab Treatments on Biliary Cirrhotic Rats. Int J Mol Sci. 2022 Jul 2;23(13):7378.