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.
IC50&Target
GLT1
5.2 mM (IC50, In rat primary neurons )
GLT1
5 nM (IC50, In human SK-N-MC cells)
体外研究
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.
体内研究
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.
分子式
C20H18F6N2O5S
分子量
512.42
CAS号
1421936-85-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 11.36 mg/mL (22.17 mM; ultrasonic and warming and heat to 60°C)