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说明： Selective GluN2A antagonist, blood-brain barrier penetrant
化学名： 5-(2-(4-Chloropyridin-2-yl)-2,2-difluoroethoxy)-6-methyl-N-(pyridin-3-ylmethyl)pyrazine-2-carboxamide
纯度： ≥98% (HPLC)
生物活性 for JNJ 78911118
JNJ 78911118 is a potent, GluN2A-selective NMDA antagonist (IC50 = 44 nM). JNJ 78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. In vitro, JNJ 78911118 promotes increases in dendritic complexity and synapse number. In vivo, JNJ 78911118 increases mEPSC frequency in rat cortical neurons, and heart rate and blood pressure in rat toxicological studies. JNJ 78911118 is orally bioavailable and blood-brain barrier penetrant.
许可信息
This compound is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the JNJ 78911118 probe summary on the SGC website.
技术数据 for JNJ 78911118
| 分子量 | 419.82 |
| 公式 | C19H16ClF2N5O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| InChI Key | YPXUKPNZQTWCRR-UHFFFAOYSA-N |
| Smiles | CC1=C(N=CC(C(NCC2=CN=CC=C2)=O)=N1)OCC(F)(C3=NC=CC(Cl)=C3)F |
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 78911118
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 41.98 | 100 | |
| ethanol | 41.98 | 100 |
制备储备液 for JNJ 78911118
以下数据基于产品分子量 419.82。 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 | 2.38 mL | 11.91 mL | 23.82 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.76 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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产品说明书 for JNJ 78911118
参考文献 for JNJ 78911118
参考文献是支持产品生物活性的出版物。
Bischoff et al (2025) Design, synthesis, and characterization of GluN2A negative allosteric modulators suitable for in vivo exploration. J.Med.Chem. 68 4672 PMID: 39960408
Lord et al (2025) Pharmacological characterisation of JNJ-78911118, a novel, centrally-penetrant, selective GluN2A antagonist. Br.J.Pharmacol. 182 4080 PMID: 40361296
If you know of a relevant reference for JNJ 78911118, please let us know.
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