Valiltramiprosate_product_DataBase

Bioactivity	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].
Target	β-amyloid
In Vivo	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].
Name	Valiltramiprosate
CAS	1034190-08-3
Formula	C8H18N2O4S
Molar Mass	238.30
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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.

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