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Merck
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Key Documents

SML2413

Sigma-Aldrich

EU1794-27

≥98% (HPLC)

同義詞:

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

經驗公式(希爾表示法):
C18H23N3O4S2
CAS號碼:
分子量::
409.52
分類程式碼代碼:
12352200

化驗

≥98% (HPLC)

形狀

powder

顏色

white to light brown

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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

生化/生理作用

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (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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