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Merck
CN

SML2992

Sigma-Aldrich

uPSEM792 hydrochloride

≥98% (HPLC)

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别名:
1-Methyl-7,8,9,10-tetrahydro-1H-6,10-methanoazepino[4,5-g]quinoxalin-2(6H)-one hydrochloride, PSEM 792 hydrochloride
经验公式(希尔记法):
C14H15N3O · HCl
分子量:
277.75
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

储存条件

desiccated

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

O=C1N(C)C2=CC(C3CNCC4C3)=C4C=C2N=C1.Cl

生化/生理作用

uPSEM792 is a selective and ultrapotent pharmacologically selective effector molecule (uPSEM) agonist for chimeric pharmacologically selective actuator modules (PSAMs) with mutant nAChR α7 ligand-binding domain (LBD) PSML181G/Q139L/Y217F (PSAM4) fused to the ion pore domain (IPD) of ligand-gated ion channels (LGICs), including glycine receptor (PSAM4-GlyR EC50 = 2.3 nM) and 5-HT3 (PSAM4-5-HT3 EC50 = 1.6 nM). uPSEM792 exhibits high PSM4 selectivity (>10,000-fold over α7-GlyR, α7-5HT3, 5HT3; >230-fold over α4β2 nAChR) and sub-nanomolar PSAM4-GlyR affinity (Ki = 0.7 nM).

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Christopher J Magnus et al.
Science (New York, N.Y.), 364(6436) (2019-03-16)
Chemogenetics enables noninvasive chemical control over cell populations in behaving animals. However, existing small-molecule agonists show insufficient potency or selectivity. There is also a need for chemogenetic systems compatible with both research and human therapeutic applications. We developed a new

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