NMDAR/TRPM4-IN-2 (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 shows neuroprotective activity. NMDAR/TRPM4-IN-2 prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC 50 of 2.1 μM. NMDAR/TRPM4-IN-2 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.
性状
Solid
体外研究(In Vitro)
NMDAR/TRPM4-IN-2 (compound 8) (0-10 μM) reduces the interactions of GluN2A and GluN2B with TRPM4 in a dose-dependent manner.NMDAR/TRPM4-IN-2 eliminates the CREB shutoff pathway and restores ERK1/2 activation and IEG induction while sparing the synaptic activity-driven, transcription-promoting activities of NMDARs. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Yan J, et al. Coupling of NMDA receptors and TRPM4 guides discovery of unconventional neuroprotectants. Science. 2020 Oct 9;370(6513):eaay3302.
溶解度数据
In Vitro: DMSO : 125 mg/mL (378.68 mM; Need ultrasonic)H2O : 100 mg/mL (302.95 mM; Need ultrasonic)配制储备液