A negative modulator of AMPA receptors containing TARP-γ8
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JNJ-55511118

Item No. 29212

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[2-chloro-6-(trifluoromethoxy)phenyl]-1,3-dihydro-2H-benzimidazol-2-one
CAS Number
2036081-86-2
Molecular Formula
C14H8ClF3N2O2
Formula Weight
328.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
ClC1=C(C2=CC(NC(N3)=O)=C3C=C2)C(OC(F)(F)F)=CC=C1
InChi Code
InChI=1S/C14H8ClF3N2O2/c15-8-2-1-3-11(22-14(16,17)18)12(8)7-4-5-9-10(6-7)20-13(21)19-9/h1-6H,(H2,19,20,21)
InChi Key
COBXSLRIXGQVGS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $103

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    10 mg

    $186

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    25 mg

    $420

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    Product Description

    JNJ-55511118 is a negative modulator of AMPA receptors containing transmembrane AMPA receptor regulatory protein γ8 (TARP-γ8).1 It inhibits glutamate-induced calcium flux in HEK293F cells co-transfected with TARP-γ8 and either GluA1o, GluA1i, GluA2i, GluA3o, or GluA4o (IC50s = 11.22, 12.3, 7.41, 38.02, and 15.85 nM, respectively). JNJ-55511118 is selective for GluA1o receptors containing TARP-γ8 over GluA1o receptors containing TARP-γ2, -γ3, -γ4, or -γ7 (IC50s = >10 μM for all). It reduces peak glutamate-induced currents in acutely dissociated murine hippocampal neurons to 60.7% of control cells when used at a concentration of 1 μM. JNJ-55511118 (1 μM) reduces field excitatory postsynaptic potentials (fEPSPs) in the hippocampal CA1 region from wild-type, but not TARP-γ8 knockout, mice. It also inhibits corneal kindling-induced seizures in mice (ED50 = 3.7 mg/kg).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Maher, M.P., Wu, N., Ravula, S., et al. Discovery and characterization of AMPA receptor modulators selective for TARP-γ8. J. Pharmacol. Exp. Ther. 357(2), 394-414 (2016).