A GlyT1 inhibitor
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Iclepertin

Item No. 41729

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[5-(methylsulfonyl)-2-[(1R)-2,2,2-trifluoro-1-methylethoxy]phenyl][(1R,5R)-1-[5-(trifluoromethyl)-3-isoxazolyl]-3-azabicyclo[3.1.0]hex-3-yl]-methanone
CAS Number
1421936-85-7
Synonyms
  • BI-425809
Molecular Formula
C20H18F6N2O5S
Formula Weight
512.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
[H][C@](C1)(C2)[C@@]1(C3=NOC(C(F)(F)F)=C3)CN2C(C4=C(O[C@@H](C(F)(F)F)C)C=CC(S(=O)(C)=O)=C4)=O
InChi Code
InChI=1S/C20H18F6N2O5S/c1-10(19(21,22)23)32-14-4-3-12(34(2,30)31)5-13(14)17(29)28-8-11-7-18(11,9-28)15-6-16(33-27-15)20(24,25)26/h3-6,10-11H,7-9H2,1-2H3/t10-,11+,18+/m1/s1
InChi Key
MYHDQTVHHMSLEF-DDBGAENHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $64

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    10 mg

    $121

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    25 mg

    $272

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    Product Description

    Iclepertin is an inhibitor of glycine transporter 1 (GlyT1; IC50s = 5 and 5.2 nM for the human and rat transporter, respectively).1 It is selective for GlyT1 over GlyT2 (IC50 = >10 µM for the human transporter). Iclepertin (0.2, 0.6, or 2 mg/kg) increases cerebrospinal fluid (CSF) levels of glycine in rats. It improves learning and memory in the social recognition test in rats when administered at doses of 0.2, 0.6, or 1.8 mg/kg.2 Iclepertin (0.5, 1.5, or 4.5 mg/kg) reverses MK-801-induced working memory deficits in the T-maze test in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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. 11(6), 616-623 (2018).

    2. 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. 382(2), 223-232 (2022).