JNJ 55511118

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Cat.No. 6278 - JNJ 55511118 | C14H8ClF3N2O2 | CAS No. 2036081-86-2
Description: Selective, high affinity 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

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. Orally bioavailable and brain penetrant. Anticonvulsant.

Licensing Information

Sold with the permission of Janssen Pharmaceutica N.V.

Technical Data

M. Wt 328.67
Formula C14H8ClF3N2O2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 2036081-86-2
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 328.67. Batch specific molecular weights may vary from batch to batch due to solvent 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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References are publications that support the products' biological activity.

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

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