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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)
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
JNJ 55511118 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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 |
| InChI Key | COBXSLRIXGQVGS-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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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Product Datasheets for JNJ 55511118
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
Do you know of a great paper that uses JNJ 55511118 from Tocris? Please let us know.
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