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Key Documents

SML3004

Sigma-Aldrich

NMDAR/TRPM4 interface inhibitor C8 dihydrochloride

≥98% (HPLC)

Synonym(s):

C8 dihydrochloride, Compound 8 dihydrochloride, N1-[(3-Bromophenyl)methyl]-N1-ethyl-1,2-ethanediamine dihydrochloride

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About This Item

Empirical Formula (Hill Notation):
C11H17BrN2·2HCl
CAS Number:
Molecular Weight:
330.09
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

powder or solid

storage condition

desiccated

color

white to beige

solubility

H2O: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

NCCN(CC)CC1=CC=CC(Br)=C1.Cl.Cl

Biochem/physiol Actions

Compound 8 (C8) is a small molecule that directly targets TRPM4 TwinF domain and blocks its interaction with GluN2A/GluN2B (NR2A/NR2B) I4 domain. C8 prevents NMDAR/TRPM4 interaction-dependent excitotoxicity (death protection EC50 = 2.1 μM 24 h post 10-min exposure of primary murine hippocampal neurons to 20 μM NMDA) without affecting, and even enhancing, NMDAR-mediated essential functions. C8 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell (RGC) loss in mice in vivo (40 mg/kg i.p. at -16h, -3h before, 0h, 3h, 24h after MCAO or 20 nmol NMDA/2.0 μL by intravitreal injection).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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Jing Yan et al.
Science (New York, N.Y.), 370(6513) (2020-10-10)
Excitotoxicity induced by NMDA receptors (NMDARs) is thought to be intimately linked to high intracellular calcium load. Unexpectedly, NMDAR-mediated toxicity can be eliminated without affecting NMDAR-induced calcium signals. Instead, excitotoxicity requires physical coupling of NMDARs to TRPM4. This interaction is

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