Iclepertin (BI-425809) 是一种有效、选择性且具有口服活性的甘氨酸转运蛋白 1 (GlyT1) 抑制剂。Iclepertin 对 GlyT2 无活性。Iclepertin 可用于阿尔茨海默病和精神分裂症研究。
货号:ajcx34854
CAS:1421936-85-7
分子式:C20H18F6N2O5S
分子量：512.42
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research[1].

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].

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].

[1]. Holger Rosenbrock, et al. Evaluation of Pharmacokinetics and Pharmacodynamics of BI 425809, a Novel GlyT1 Inhibitor: Translational Studies. Clin Transl Sci. 2018 Nov;11(6):616-623.