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NMDAR/TRPM4 inhibitor 8

Names

[ CAS No. ]:
1353979-43-7

[ Name ]:
NMDAR/TRPM4 inhibitor 8

[Synonym ]:
N-(3-Bromobenzyl)-N-ethyl-1,2-ethanediamine
1,2-Ethanediamine, N1-[(3-bromophenyl)methyl]-N1-ethyl-
MFCD21096961
NMDAR/TRPM4 inhibitor 8

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR
Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel
Signaling Pathways >> MAPK/ERK Pathway >> ERK
Research Areas >> Neurological Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR
Signaling Pathways >> Stem Cell/Wnt >> ERK

[In Vitro]

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].

[References]

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

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
300.6±22.0 °C at 760 mmHg

[ Molecular Formula ]:
C11H17BrN2

[ Molecular Weight ]:
257.17

[ Flash Point ]:
135.6±22.3 °C

[ Exact Mass ]:
256.057495

[ LogP ]:
2.40

[ Vapour Pressure ]:
0.0±0.6 mmHg at 25°C

[ Index of Refraction ]:
1.564

Safety Information

[ Hazard Codes ]:
C

Related Compounds