SML3004
NMDAR/TRPM4 interface inhibitor C8 dihydrochloride
≥98% (HPLC)
别名:
C8 dihydrochloride, Compound 8 dihydrochloride, N1-[(3-Bromophenyl)methyl]-N1-ethyl-1,2-ethanediamine dihydrochloride
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关于此项目
经验公式（希尔记法）:
C11H17BrN2·2HCl
化学文摘社编号:
分子量:
330.09
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
NMDAR/TRPM4 interface inhibitor C8 dihydrochloride, ≥98% (HPLC)
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
InChI key
AQDSZKTVQVSVNC-UHFFFAOYSA-N
SMILES string
NCCN(CC)CC1=CC=CC(Br)=C1.Cl.Cl
assay
≥98% (HPLC)
form
powder or solid
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
−20°C
Quality Level
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).
TRPM4 TwinF domain-targeting NMDAR/TRPM4 interaction blocker that protects against TRPM4-mediated excitotoxicity in vitro and in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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