化合物 Iclepertin T37089

Product Introduction
Bioactivity


英文名: Iclepertin

描述: Iclepertin (BI-425809) is a highly effective, selective, and orally bioavailable inhibitor of glycine transporter 1 (GlyT1). It exhibits no activity against GlyT2. Consequently, Iclepertin holds promise for advancing research on Alzheimer's disease and schizophrenia [1].

体外活性: Iclepertin inhibits GlyT1 with the IC50 values of 5.2 nM in rat primary neurons and 5.0 nM in human SK-N-MC cells[1].

体内活性: Single oral administration of Iclepertin induced a dose-dependent increase of glycine cerebrospinal fluid (CSF) levels. Oral administration of Iclepertin in rats induced a dose‐dependent increase of glycine CSF levels from 30% (0.2 mg/kg, not significant) to 78% (2 mg/kg), relative to vehicle[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: Iclepertin

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途