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Merck
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Key Documents

Altri documenti

SML2413

Sigma-Aldrich

EU1794-27

≥98% (HPLC)

Sinonimo/i:

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

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About This Item

Formula empirica (notazione di Hill):
C18H23N3O4S2
Numero CAS:
1832671-21-2
Peso molecolare:
409.52
Codice UNSPSC:
12352200

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to light brown

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

2-8°C

Stringa SMILE

O=C(C(CC(NC1=C(C(OC(C)(C)C)=O)C2=C(CCCC2)S1)=O)S3)NC3=N

Azioni biochim/fisiol

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).
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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

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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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