ALZ-801 是一种口服可用的小分子 β-淀粉样蛋白 β-amyloid (Aβ) 抑制剂， Tramiprosate 缬氨酸偶联前药，有显著改善的 PK 特性和胃肠耐受性。ALZ-801 有潜力用于研究阿尔茨海默病的研究。
货号:ajcx34502
CAS:1034190-08-3
分子式:C8H18N2O4S
分子量：238.3
溶解度:H2O : 250 mg/mL (1049.10 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound[1]. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease[2].

ALZ-801 (oral administration; 172 mg/kg; single dose) exhibits mean AUCt values of 58,758 and 5841 ng/ml.h in plasma and brain, respectively. The ALZ-801: Tramiprosate ratio in plasma and brain is 1.8 and 3.1, respectively in male CD-1 mice[1].

[1]. John A. Hey, et al. Discovery and Identification of an Endogenous Metabolite of Tramiprosate and Its Prodrug ALZ-801 that Inhibits Beta Amyloid Oligomer Formation in the Human Brain. CNS Drugs. 2018; 32(9): 849-861.
[2]. Hey JA, et al. Clinical Pharmacokinetics and Safety of ALZ-801, a Novel Prodrug of Tramiprosate in Development for the Treatment of Alzheimer’s Disease. Clin Pharmacokinet. 2018 Mar;57(3):315-333.