JNJ-61432059是具有口服活性的、选择性的AMPAR的负向调节剂，其对GluA1/γ-8的pIC50值为9.7。在老鼠的海马体中显示出具有时间和剂量依赖性的AMPA受体占用情况，在角膜点燃癫痫动物模型中显示出较强的保护作用。
| Cas No. | 2035814-50-5 |
| Canonical SMILES | OC1CCN(C2=NC=CC3=C(C4=CC=C(NC(C5)=O)C5=C4)C(C6=CC=C(F)C=C6)=NN32)CC1 |
| 分子式 | C25H22FN5O2 |
| 分子量 | 443.47 |
| 溶解度 | DMSO: 50 mg/mL (112.75 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models[1].
pIC50: 9.7 (AMPAR)[1]. [1]. Savall BM, et al. Discovery of Imidazo[1,2-a]pyrazines and Pyrazolo[1,5-c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators. ACS Med Chem Lett. 2018 Dec 26;10(3):267-272. |
