Iclepertin,1421936-85-7

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Iclepertin

CAS No. : 1421936-85-7

MCE 国际站：Iclepertin

产品活性：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。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：GlyT

In Vitro: 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.

In Vivo: 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.

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