ALZ-801 是一种可口服的小分子 β-淀粉样蛋白抗寡聚体和聚集抑制剂,是曲米酸的缬氨酸偶联前药,与母体化合物相比,具有显著改善的 PK 特性和胃肠道耐受性。它是治疗阿尔茨海默病的先进且显著改善的候选药物。
产品描述
ALZ-801 is an orally available, valine-conjugated prodrug of tramiprosate. ALZ-801 is an advanced and markedly improved candidate for the treatment of Alzheimer's disease. ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, a valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound.
体内活性
The ALZ-801: Tramiprosate ratio in plasma and brain is 1.8 and 3.1, respectively in male CD-1 mice[1]. ALZ-801 (oral administration; 172 mg/kg; single dose) shows average AUCt values of 58,758 and 5841 ng/ml.h in plasma and brain, respectively.
Cas No.
1034190-08-3
分子式
C8H18N2O4S
分子量
238.31
储存和溶解度
H2O:250 mg/mL (1049.10 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years