NMDAR/TRPM4-IN-2( —— )

Catalog No. M36470 CAS No. 2243506-33-2

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

NMDAR/TRPM4-IN-2
Note

Research use only, not for human use.
Brief Description

NMDAR/TRPM4-IN-2 is a potent interfacial inhibitor of NMDAR/TRPM4 interaction.NMDAR/TRPM4-IN-2 protects against MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss in mice.
Description

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.
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.
In Vivo

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Synonyms

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Pathway

MAPK/ERK Signaling
Target

ERK
Recptor

ERK | TRP/TRPV Channel | iGluR | NMDAR
Research Area

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Indication

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CAS Number

2243506-33-2
Formula Weight

330.092
Molecular Formula

C11H19BrCl2N2
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 250 mg/mL (757.37 mM; Ultrasonic ) H2O : 100 mg/mL (302.95 mM; Ultrasonic)
SMILES

Cl.Cl.CCN(CCN)Cc1cccc(Br)c1
Chemical Name

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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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