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Merck
모든 사진(1)

주요 문서

SML2412

Sigma-Aldrich

EU1794-4

≥98% (HPLC)

동의어(들):

2-[[(2-Amino-4,5-dihydro-4-oxo-5-thiazolyl)acetyl]amino]-4,5,6,7-tetrahydro-1-benzo[b]thiophene-3-carboxylic acid ethyl ester, 2-[[(2-Imino-4-oxo-1,3-thiazolidin-5-yl)acetyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxylic acid ethyl ester, EU 1794-4, Ethyl 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

실험식(Hill 표기법):
C16H19N3O4S2
CAS Number:
Molecular Weight:
381.47
MDL number:
UNSPSC 코드:
12352200

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

SMILES string

O=C(OCC)C1=C(SC2=C1CCCC2)NC(CC3SC(NC3=O)=N)=O

생화학적/생리학적 작용

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).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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시험 성적서(COA)

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문서 라이브러리 방문

Brooke M Katzman et al.
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An NMDAR positive and negative allosteric modulator series share a binding site and are interconverted by methyl groups
Perszyk R, et al.
eLife, 7, e34711-e34711 (2018)
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Bioorganic & medicinal chemistry letters, 19(22), 6337-6339 (2009-10-13)
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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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