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经验公式(希尔记法):
C16H19N3O4S2
化学文摘社编号:
分子量:
381.47
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.21
产品名称
EU1794-4, ≥98% (HPLC)
SMILES string
O=C(OCC)C1=C(SC2=C1CCCC2)NC(CC3SC(NC3=O)=N)=O
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
Allosteric NMDAR modulator that reduces or augments receptor activation, respectively, in the presence of high or low Glu/Gly levels.
EU1794-4 consists of an ethyl ester and lacks a methyl substituent on the tetrahydrobenzothiophene core.
EU1794-4 is an N-methyl-d-aspartate (NMDA) receptor (NMDAR) allosteric modulator that prevents large degree receptor activation in the presence of high level Glu/Gly (IC50/Emax = 2.2 μM/32%/GluN2A, 2.6 μM/67%/GluN2B, 0.42 μM/52%/GluN2C, 0.36 μM/51%/GluN2D with Glu/Gly = ECmax = 100/30 μM using xenopus oocytes co-expressing rat GluN1 and respective GluN2 subtype), while augmenting receptor activation at low level Glu/Gly (EC50/Emax = 3.9 μM/500%/GluN2A, 4.3 μM/210%/GluN2B, 15 μM/220%/GluN2C with Glu/Gly = 1/0.3 μM; 14 μM/540%/GluN2D with Glu/Gly = 300/9 nM).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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Perszyk R, et al.
eLife, 7, e34711-e34711 (2018)
Riley Perszyk et al.
eLife, 7 (2018-05-25)
N-methyl-d-aspartate receptors (NMDARs) are an important receptor in the brain and have been implicated in multiple neurological disorders. Many non-selective NMDAR-targeting drugs are poorly tolerated, leading to efforts to target NMDAR subtypes to improve the therapeutic index. We describe here
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