JNJ 55511118
Tocris Bioscience, part of Bio-Techne | Catalog # 6278
High affinity and selective negative modulator of AMPA receptors containing TARP-γ8
Key Product Details
Description
High affinity and selective negative modulator of AMPA receptors containing TARP-γ8
Product Description
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.Product Specifications
Molecular Weight
328.67
Formula
C14H8ClF3N2O2
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
5-[2-Chloro-6-(trifluoromethoxy)phenyl]-1,3-dihydro-2H-benzimidazol-2-one
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.
Solubility
| 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 all 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 | 0.30 mL | 1.52 mL | 3.04 mL |
| 50 mM | 0.06 mL | 0.30 mL | 0.61 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Witkin A Comment on "Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8". J.Pharmacol.Exp.Ther. 2016 PMID: 27528544
- Hoffman 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. 2021 PMID: 34086361
- Maher Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8. J.Pharmacol.Exp.Ther. 2016 PMID: 26989142
Product Specific Notices for JNJ 55511118
For research use only
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