A negative modulator of AMPA receptors containing TARP-γ8; inhibits glutamate-induced calcium flux in HEK293F cells co-transfected with TARP-γ8 and either GluA1o

JNJ-55511118 – 1 mg

Brand:
Cayman
CAS:
2036081-86-2
Storage:
-20
UN-No:
Non-Hazardous - /

JNJ-55511118 is a negative modulator of AMPA receptors containing transmembrane AMPA receptor regulatory protein γ8 (TARP-γ8).{48698} 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).  

 

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Description

A negative modulator of AMPA receptors containing TARP-γ8; 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); selective for GluA1o receptors containing TARP-γ8 over GluA1o receptors containing TARP-γ2, -γ3, -γ4, or -γ7 (IC50s = >10 μM for all); reduces peak glutamate-induced currents in acutely dissociated murine hippocampal neurons to 60.7% of control cells at 1 μM; reduces fEPSPs in the hippocampal CA1 region from wild-type, but not TARP-γ8 knockout, mice at 1 μM; inhibits corneal kindling-induced seizures in mice (ED50 = 3.7 mg/kg)

Formal name: 5-[2-chloro-6-(trifluoromethoxy)phenyl]-1,3-dihydro-2H-benzimidazol-2-one

Synonyms: 

Molecular weight: 328.7

CAS: 2036081-86-2

Purity: ≥98%

Formulation: A crystalline solid

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