SML2413
EU1794-27
≥98% (HPLC)
别名:
2-[[(2-Amino-4,5-dihydro-4-oxo-5-thiazolyl)acetyl]amino]-4,5,6,7-tetrahydro-1-benzo[b]thiophene-3-carboxylic acid tert-butyl ester, 2-[[(2-Imino-4-oxo-1,3-thiazolidin-5-yl)acetyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxylic acid tert-butyl ester, EU 1794-27, Tert-butyl 2-(2-(2-imino-4-oxothiazolidin-5-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate
产品名称
EU1794-27, ≥98% (HPLC)
SMILES string
O=C(C(CC(NC1=C(C(OC(C)(C)C)=O)C2=C(CCCC2)S1)=O)S3)NC3=N
assay
≥98% (HPLC)
form
powder
color
white to light brown
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
EU1794-27 is an N-methyl-d-aspartate (NMDA) receptor (NMDAR) positive allosteric modulator (PAM) toward GluN2A/B/C subtypes (EC50/Emax = 1.4 μM/130%/GluN2B, 2.8 μM/230%/GluN2C, 2.4 μM/250%/GluN2D with Glu/Gly = ECmax = 100/30 μM using xenopus oocytes co-expressing rat GluN1 and respective GluN2 subtype; EC50/Emax = 6.3 μM/400%/GluN2B, 5.0 μM/680%/GluN2C with Glu/Gly = 1/0.3 μM &,;2.4 μM/580%/GluN2D with Glu/Gly = 0.6/0.2 μM), while it exhibits Glu/Gly level-dependent GluN1-GluN2A-modulating activities (EC50/Emax = 7.4 μM/52%/GluN2A with Glu/Gly = 100/30 μM; 8.1 μM/340% with Glu/Gly = 2/0.6 μM).
GluN2B/C/D NMDAR positive allosteric modulator with Glu/Gly level-dependent modulating activity toward GluN2A.
NMDA receptor is important for glutamate neurotransmission. It is associated with learning ability and memory. NMDA receptor possesses two different subunits NMDAR1 and NMDAR2. Tyrosine phosphorylation controls the actions of NMDA receptors. It is also known to influence neuronal function.
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
PSD-95 promotes Fyn-mediated tyrosine phosphorylation of the N-methyl-D-aspartate receptor subunit NR2A
Tezuka T, et al.
Proceedings of the National Academy of Sciences of the USA, 96(2), 435-440 (1999)
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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