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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-iGluR-Blixeprodil
Blixeprodil

Chemical Structure : Blixeprodil

CAS No.: 2881017-49-6

Blixeprodil (GM-1020, GM1020)

货号: PC-24115Not For Human Use, Lab Use Only.

Blixeprodil (GM-1020) is a selective NMDA receptor (NMDAR) antagonist, displaces [3H]MK-801 binding to NMDAR in rat cortical tissue with Ki of 3.25 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Blixeprodil (GM-1020) is a selective NMDA receptor (NMDAR) antagonist, displaces [3H]MK-801 binding to NMDAR in rat cortical tissue with Ki of 3.25 uM.
GM-1020 shows no binding affinity for AMPA, melanocortin 4, and α4β2 nicotinic acetylcholine receptors, and no agonist activity at the 5-HT1B receptor.
GM-1020 showed functional inhibition of NMDAR-mediated currents in NR2A- and NR2B-containing receptors, with IC50 values of 3.70 µM and 4.16 µM, respectively.
GM-1020 showed functional inhibition of NR1/2A-NMDAR-mediated currents with IC50 of 1.192 µM in HEK cells.
GM-1020 shows rapid and robust antidepressant-like effects.

物理化学性质&存储条件

分子量 221.28
分子式 C13H16FNO
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2R)-2-(4-fluorophenyl)-2-(methylamino)cyclohexan-1-one

参考文献

1. Klein AK, et al. Neuropsychopharmacology. 2024 May;49(6):905-914.

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