JNJ 55511118

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Description: High affinity and selective negative modulator of AMPA receptors containing TARP-γ8
Chemical Name: 5-[2-Chloro-6-(trifluoromethoxy)phenyl]-1,3-dihydro-2H-benzimidazol-2-one
Purity: ≥98% (HPLC)
Citations (2)
Literature (5)

Biological Activity for JNJ 55511118

JNJ 55511118 is a high affinity and selective negative modulator of AMPA receptors containing TARP-γ8 (Ki = 26 nM). Exhibits <50% binding against a panel of 52 receptors, ion channels and transporters (except 5HT2B and melatonin receptors 78% and 57%, respectively). Also displays minimal activity against other TARP-less AMPARs and AMPARs coexpressed with other TARPs or CNIH2. It reduces alcohol self-administration in a mouse models of chronic drinking. Orally bioavailable and brain penetrant. Anticonvulsant.

Licensing Information

Sold with the permission of Janssen Pharmaceutica N.V.

Compound Libraries for JNJ 55511118

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Technical Data for JNJ 55511118

M. Wt 328.67
Formula C14H8ClF3N2O2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 2036081-86-2
PubChem ID 122656423
Smiles ClC1=CC=CC(OC(F)(F)F)=C1C2=CC=C3NC(NC3=C2)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for JNJ 55511118

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 32.87 100
ethanol 32.87 100

Preparing Stock Solutions for JNJ 55511118

The following data is based on the product molecular weight 328.67. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.04 mL 15.21 mL 30.43 mL
5 mM 0.61 mL 3.04 mL 6.09 mL
10 mM 0.3 mL 1.52 mL 3.04 mL
50 mM 0.06 mL 0.3 mL 0.61 mL

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References for JNJ 55511118

References are publications that support the biological activity of the product.

Maher et al (2016) Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8. J.Pharmacol.Exp.Ther. 357 394 PMID: 26989142

Witkin et al (2016) A Comment on "Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8". J.Pharmacol.Exp.Ther. 358 502 PMID: 27528544

Hoffman (2021) Inhibition of AMPA receptors (AMPARs) containing transmembrane AMPAR regulatory protein γ-8 with JNJ-55511118 shows preclinical efficacy in reducing chronic repetitive alcohol self-administration. Alcohol Clin.Exp.Res. 45 1424 PMID: 34086361

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Keywords: JNJ 55511118, JNJ 55511118 supplier, JNJ55511118, High, affinity, selective, negative, modulators, modulates, AMPA, receptors, containing, TARP-gamma8, TARP-γ8, Receptors, 6278, Tocris Bioscience

2 Citations for JNJ 55511118

Citations are publications that use Tocris products. Selected citations for JNJ 55511118 include:

Hoffman et al (2021) Inhibition of AMPA receptors (AMPARs) containing transmembrane AMPAR regulatory protein γ-8 with JNJ-55511118 shows preclinical efficacy in reducing chronic repetitive alcohol self-administration. Alcohol Clin.Exp.Res. 45 1424 PMID: 34086361

Richard D et al (2022) NMDAR-dependent presynaptic homeostasis in adult hippocampus: Synapse growth and cross-modal inhibitory plasticity. Neuron 110 3302-3317.e7 PMID: 36070750

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Literature in this Area

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