Iclepertin (Synonyms: BI-425809) |
Catalog No.GC63014
One-Click Copy Product Info
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Iclepertin is a selective glycine transporter 1 (GlyT1) inhibitor that functions by inhibiting GlyT1, thereby modulating intracellular glycine concentration.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1421936-85-7
Sample solution is provided at 25 µL, 10mM.
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Iclepertin is a selective glycine transporter 1 (GlyT1) inhibitor that functions by inhibiting GlyT1, thereby modulating intracellular glycine concentration[1-2]. Iclepertin is used in research related to cognitive impairment associated with schizophrenia (CIAS) and Alzheimer's disease[3-4].
In vivo, in a schizophrenia-associated mouse model using C57BL/6JRj mice, Iclepertin (0.3, 1, or 4mg/kg; subcutaneous injection) administered 15 minutes before MK-801 treatment. Iclepertin significantly reversed MK-801-induced deficits in auditory event-related potential N1 amplitude and N1 gating, as well as reductions in 40Hz auditory steady-state response power and intertrial coherence, while also suppressing abnormal basal gamma power elevation. In CD-1 mice treated with MK-801, Iclepertin (0.5, 1.5, or 4.5mg/kg; oral administration) given 60 minutes before behavioral testing. Iclepertin significantly improved working memory deficits and increased spontaneous alternation accuracy. In untreated Wistar rats performing a social recognition task, a single dose of Iclepertin (0.2, 0.6, or 1.8mg/kg; oral administration) administered 60 minutes before training and testing. Iclepertin significantly reduced social investigation time after a 24-hour delay and enhanced social recognition memory performance[5]. Iclepertin (0.2, 0.6, or 2mg/kg; oral administration) administered as a single dose to Wistar rats. Iclepertin resulted in a dose-dependent increase in cerebrospinal fluid glycine levels when measured 90 minutes post-administration[6].
References:
[1] Li N, Wei Y, Li R, et al. Modulation of the human GlyT1 by clinical drugs and cholesterol. Nat Commun. 2025 Mar 11;16(1):2412.
[2] Keefe RSE, Harvey PD, Correll CU, et al. Efficacy and safety of iclepertin for cognitive impairment associated with schizophrenia (CONNEX programme): results from three phase 3 randomised controlled trials. Lancet Psychiatry. 2025 Dec;12(12):906-920.
[3] Rosenbrock H, Desch M, Wunderlich G. Development of the novel GlyT1 inhibitor, iclepertin (BI 425809), for the treatment of cognitive impairment associated with schizophrenia. Eur Arch Psychiatry Clin Neurosci. 2023 Oct;273(7):1557-1566.
[4] Ye N, Wang Q, Li Y, et al. Current emerging therapeutic targets and clinical investigational agents for schizophrenia: Challenges and opportunities. Med Res Rev. 2025 Mar;45(2):755-787.
[5] Rosenbrock H, Dorner-Ciossek C, Giovannini R, et al. Effects of the Glycine Transporter-1 Inhibitor Iclepertin (BI 425809) on Sensory Processing, Neural Network Function, and Cognition in Animal Models Related to Schizophrenia. J Pharmacol Exp Ther. 2022 Aug;382(2):223-232.
[6] Rosenbrock H, Desch M, Kleiner O, 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.
| Animal experiment [1]: | |
Animal models | C57BL/6JRj mice (12–14 weeks old) and CD-1 mice (4–5 weeks old) for EEG/cognition studies; adult male Wistar rats (12–15 weeks old) for social recognition task |
Preparation Method | EEG/sensory processing: Mice were subcutaneously administered Iclepertin (0.3, 1, or 4mg/kg) 15 minutes before MK-801 (0.15mg/kg; s.c.) or vehicle; EEG recordings (AERP, ASSR, basal/evoked gamma oscillations) were performed in prefrontal cortex (PFC) and auditory cortex (AC). T-maze spontaneous alternation (mice): Iclepertin (0.5–4.5mg/kg; p.o.) was administered 60 minutes before MK-801 (0.1mg/kg; s.c.); working memory was assessed via spontaneous alternation percentage. Social recognition (rats): Iclepertin (0.2, 0.6, or 1.8mg/kg; p.o.) was given 60 minutes before T1 (training) and T2 (24-hour retention test); social investigation time reduction indicated memory improvement. |
Dosage form | 0.3–4.5mg/kg; s.c./p.o.; acute or subchronic dosing. |
Applications | Iclepertin significantly reversed MK-801-induced deficits in auditory event-related potentials and 40Hz auditory steady-state response in PFC and AC. Iclepertin attenuated MK-801-induced increases in basal gamma power, indicating normalized cortical network excitability. Iclepertin restored working memory in MK-801-treated mice and enhanced social recognition memory in naïve rats. |
References: | |
| Cas No. | 1421936-85-7 | SDF | |
| Synonyms | BI-425809 | ||
| Formula | C20H18F6N2O5S | M.Wt | 512.42 |
| Solubility | DMSO : 11.36 mg/mL (22.17 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9515 mL | 9.7576 mL | 19.5152 mL |
| 5 mM | 390.3 μL | 1.9515 mL | 3.903 mL |
| 10 mM | 195.2 μL | 975.8 μL | 1.9515 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)