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
质量水平
方案
≥98% (HPLC)
表单
powder or solid
储存条件
desiccated
颜色
white to beige
溶解性
H2O: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
NCCN(CC)CC1=CC=CC(Br)=C1.Cl.Cl
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
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).
TRPM4 TwinF domain-targeting NMDAR/TRPM4 interaction blocker that protects against TRPM4-mediated excitotoxicity in vitro and in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°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
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持