SML3004
NMDAR/TRPM4 interface inhibitor C8 dihydrochloride
≥98% (HPLC)
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Synonym(s):
C8 dihydrochloride, Compound 8 dihydrochloride, N1-[(3-Bromophenyl)methyl]-N1-ethyl-1,2-ethanediamine dihydrochloride
Empirical Formula (Hill Notation):
C11H17BrN2·2HCl
CAS Number:
Molecular Weight:
330.09
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
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).
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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