Bioactivity | 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]. | ||||||||||||
Target | pIC50: 9.7 (AMPAR). | ||||||||||||
Name | JNJ-61432059 | ||||||||||||
CAS | 2035814-50-5 | ||||||||||||
Formula | C25H22FN5O2 | ||||||||||||
Molar Mass | 443.47 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |