An inhibitor of GlyT1
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Bitopertin

Item No. 19896

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[4-[3-fluoro-5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl][5-(methylsulfonyl)-2-[(1S)-2,2,2-trifluoro-1-methylethoxy]phenyl]-methanone
CAS Number
845614-11-1
Synonyms
  • RG-1678
  • RO-4917838
Molecular Formula
C21H20F7N3O4S
Formula Weight
543.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2)(1:12): 0.25 mg/mlDMSO: 25 mg/mlEthanol: 5 mg/ml
λmax
243, 254, 299 nm
SMILES
FC1=C(N2CCN(C(C3=C(O[C@H](C(F)(F)F)C)C=CC(S(C)(=O)=O)=C3)=O)CC2)N=CC(C(F)(F)F)=C1
InChi Code
InChI=1S/C21H20F7N3O4S/c1-12(20(23,24)25)35-17-4-3-14(36(2,33)34)10-15(17)19(32)31-7-5-30(6-8-31)18-16(22)9-13(11-29-18)21(26,27)28/h3-4,9-12H,5-8H2,1-2H3
InChi Key
YUUGYIUSCYNSQR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $134

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    25 mg

    $316

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    50 mg

    $598

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    100 mg

    $1,058

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    Product Description

    Bitopertin is an inhibitor of glycine transporter 1 (GlyT1; IC50 = 0.03 µM).1 It is selective for GlyT1 over GlyT2 (IC50 = >30 µM) as well as a panel of 107 receptors, transporters, and enzymes at 10 µM.1,2 Bitopertin (0.1 µM) increases long-term potentiation in rat hippocampal CA1 slices.2 It reverses hyperlocomotion induced by the NMDA receptor partial agonist L-687,414 in mice (ID50 = 0.5 mg/kg).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pinard, E., Alanine, A., Alberati, D., et al. Selective GlyT1 inhibitors: Discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia. J. Med. Chem. 53(12), 4603-4614 (2010).

    2. Alberati, D., Moreau, J.-L., Lengyel, J., et al. Glycine reuptake inhibitor RG1678: A pharmacologic characterization of an investigational agent for the treatment of schizophrenia. Neuropharmacology 62(2), 1152-1161 (2012).