NMDAR/TRPM4-IN-2 free base (化合物 8) 是一种有效的 NMDAR/TRPM4 相互作用界面抑制剂。NMDAR/TRPM4-IN-2 free base 具有神经保护活性。NMDAR/TRPM4-IN-2 free base 可预防 NMDA 诱导的海马神经元细胞死亡和线粒体功能障碍，其 IC50 值为 2.1 μM。NMDAR/TRPM4-IN-2 free base 保护小鼠免受 MCAO 诱导的脑损伤和 NMDA 诱导的视网膜神经节细胞丢失。
货号:ajcx37776
CAS:1353979-43-7
分子式:C11H17BrN2
分子量：257.17
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

NMDAR/TRPM4-IN-2 free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 free base shows neuroprotective activity. NMDAR/TRPM4-IN-2 free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss[1].

NMDAR/TRPM4-IN-2 free base (compound 8) (0-10 μM) reduces the interactions of GluN2A and GluN2B with TRPM4 in a dose-dependent manner[1].NMDAR/TRPM4-IN-2 free base eliminates the CREB shutoff pathway and restores ERK1/2 activation and IEG induction while sparing the synaptic activity-driven, transcription-promoting activities of NMDARs[1].

[1]. Yan J, et al. Coupling of NMDA receptors and TRPM4 guides discovery of unconventional neuroprotectants. Science. 2020 Oct 9;370(6513):eaay3302.