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].

1421936-85-7

C20H18F6N2O5S

512.42

Iclepertin

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years