PeptideDB

NMDAR/TRPM4-IN-2

CAS: 2243506-33-2 F: C11H19BrCl2N2 W: 330.09

NMDAR/TRPM4-IN-2 (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 shows neuroprote
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Bioactivity 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 IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss[1].
Invitro NMDAR/TRPM4-IN-2 (compound 8) (0-10 μM) reduces the interactions of GluN2A and GluN2B with TRPM4 in a dose-dependent manner[1].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[1].
Name NMDAR/TRPM4-IN-2
CAS 2243506-33-2
Formula C11H19BrCl2N2
Molar Mass 330.09
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

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)

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