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Submit ReviewJNJ 55511118
说明： High affinity and selective negative modulator of AMPA receptors containing TARP-γ8
化学名： 5-[2-Chloro-6-(trifluoromethoxy)phenyl]-1,3-dihydro-2H-benzimidazol-2-one
纯度： ≥98% (HPLC)
生物活性 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.
许可信息
Sold with the permission of Janssen Pharmaceutica N.V.
化合物库 for JNJ 55511118
JNJ 55511118 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for JNJ 55511118
| 分子量 | 328.67 |
| 公式 | C14H8ClF3N2O2 |
| 储存 | Store at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for JNJ 55511118
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 32.87 | 100 | |
| ethanol | 32.87 | 100 |
制备储备液 for JNJ 55511118
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for JNJ 55511118
参考文献 for JNJ 55511118
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for JNJ 55511118, please let us know.
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关键词: JNJ 55511118, JNJ 55511118 supplier, JNJ55511118, High, affinity, selective, negative, modulators, modulates, AMPA, receptors, containing, TARP-gamma8, TARP-γ8, Receptors, 6278, Tocris Bioscience
2 篇 JNJ 55511118 的引用文献
引用文献是使用了 Tocris 产品的出版物。 JNJ 55511118 的部分引用包括：
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
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
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