Aliskiren

国际站：Aliskiren

中文名：阿利克仑

CAS：173334-57-1

品牌：MedChemExpress (MCE)

存储条件：Pure form: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性：Aliskiren 是一种具有口服活性、高效且选择性的 renin 抑制剂，IC₅₀ 为 1.5 nM。阿利吉仑可用于高血压、心血管疾病和癌症恶病质的研究^[1][2][3]。 IC50 和目标：IC50：1.5 nM（肾素）。

体内：阿利吉仑（< 10 mg/kg，口服，每日）抑制钠耗尽狨猴的血浆肾素活性并降低血压^[2]。阿利吉仑（10 mg/kg，灌胃，一次) 显着减轻携带 C26 小鼠结肠癌细胞的 BALB/c 小鼠的多种恶病质相关症状，包括 BW 损失、肿瘤负荷、肌肉萎缩、肌肉功能障碍和缩短的生存期^[3]。

参考文献：[1]. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754–758[2]. Buczko W, et al. Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin inhibitor. Pharmacol Rep. 2008 Sep-Oct;60(5):623-31.[3]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor.Biochem Biophys Res Commun, 2003, 308(4), 698-705.[4]. Gradman AH, et al.Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation, 2005, 111(8), 1012-1018.[5]. Chang AY, et al. Interplay between brain stem angiotensins and monocyte chemoattractant protein-1 as a novel mechanism for pressor response after ischemic stroke. Neurobiol Dis. 2014 Nov;71:292-304.[6]. Wang C, et al. Aliskiren targets multiple systems to alleviate cancer cachexia. Oncol Rep. 2016 Nov;36(5):3014-3022.