| Description | Iclepertin (BI-425809) is an orally active and selective inhibitor of glycine transporter protein 1 (GlyT1).Iclepertin is used for the treatment of central nervous system disorders such as Alzheimer;s disease. Iclepertin is used for central nervous system disorders such as Alzheimer;s disease, schizophrenia and cognitive disorders. |
| In vitro | Iclepertin 作为 GlyT1 的抑制剂 ，其在大鼠原代神经元和人 SK-N-MC 细胞中的 IC50 值分别为 5.2 nM和 5.0 nM[1]。 |
| In vivo | 在大鼠中口服 Iclepertin(BI 425809)诱导甘氨酸脑脊液水平从30%（0.2 mg/kg）到 78%（2 mg/kg）的剂量依赖性增加[1]。 |
| Target activity | GLT1:5.2 mM (rat primary neurons), GLT1:5 nM (human SK-N-MC cells) |
| Synonyms | BI-425809 |
| molecular weight | 512.42 |
| Molecular formula | C20H18F6N2O5S |
| CAS | 1421936-85-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 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. |