| Description | 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. |
| In vivo | ALZ-801与Tramiprosate在雄性CD-1小鼠的血浆和大脑中的比例分别为1.8和3.1[1]。经口给予ALZ-801（单剂量；172 mg/kg）后，在血浆和大脑中的平均AUCt值分别为58,758和5841 ng/ml.h。 |
| Synonyms | Valiltramiprosate |
| molecular weight | 238.3 |
| Molecular formula | C8H18N2O4S |
| CAS | 1034190-08-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: < 1 mg/mL (insoluble or slightly soluble) H2O: 20 mg/ml (83.93 mM), Sonication is recommended. |
| References | 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. |