NMDAR/TRPM4-IN-2

• CAT Number: I042012
• CAS Number: 2243506-33-2
• Molecular Formula: C11H19BrCl2N2
• Molecular Weight: 330.09
• Purity: ≥95%
• Synonyms: N’-[(3-bromophenyl)methyl]-N’-ethylethane-1,2-diamine;dihydrochloride
• InChI: InChI=1S/C11H17BrN2.2ClH/c1-2-14(7-6-13)9-10-4-3-5-11(12)8-10;;/h3-5,8H,2,6-7,9,13H2,1H3;2*1H
• InChIKey: AQDSZKTVQVSVNC-UHFFFAOYSA-N
• SMILES: CCN(CCN)CC1=CC(=CC=C1)Br.Cl.Cl

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].
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].

Reference

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