| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| 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[1]. | ||||||||||||
| Name | Iclepertin | ||||||||||||
| CAS | 1421936-85-7 | ||||||||||||
| Formula | C20H18F6N2O5S | ||||||||||||
| Molar Mass | 512.42 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Iclepertin
CAS: 1421936-85-7 F: C20H18F6N2O5S W: 512.42
Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is i
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