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Merck
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文件

SML3004

Sigma-Aldrich

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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About This Item

经验公式（希尔记法）:
C11H17BrN2·2HCl
CAS号:
2243506-33-2
分子量:
330.09
MDL號碼:
MFCD31668685
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder or solid

儲存條件

desiccated

顏色

white to beige

溶解度

H2O: 2 mg/mL, clear

儲存溫度

−20°C

SMILES 字串

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

生化／生理作用

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).

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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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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