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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-iGluR-MPX-004
MPX-004

Chemical Structure : MPX-004

CAS No.: 1688684-07-2

MPX-004 (MPX004)

货号: PC-23361Not For Human Use, Lab Use Only.

MPX-004 is a potent, GluN2A-selective negative allosteric modulator and NMDA antagonist with IC50 of 78 nM for inhibition of Ca2+ responses mediated by GluN2A receptors expressed in HEK cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MPX-004 is a potent, GluN2A-selective negative allosteric modulator and NMDA antagonist with IC50 of 78 nM for inhibition of Ca2+ responses mediated by GluN2A receptors expressed in HEK cells.
MPX-004 inhibits NMDA receptor-mediated currents in Xenopus oocytes expressing human GluN1 + GluN2A with IC50 of 198 nM.
MPX-004 only weakly (up to 8%) inhibited currents in oocytes expressing GluN2B, C, or D receptors up to 10 uM.
MPX-004 potently inhibits NMDA/glycine-induced currents of rat cortical neurons in primary culture.
MPX-004 reduces the ratio of NMDA receptor- to AMPA receptor-mediated synaptic currents (NMDAR/AMPAR ratio) at layer 4-to-2/3 synapses in mouse visual cortex.

物理化学性质&存储条件

分子量 455.91
分子式 C17H15ClFN5O3S2
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

5-(((3-chloro-4-fluorophenyl)sulfonamido)methyl)-N-((2-methylthiazol-5-yl)methyl)pyrazine-2-carboxamide

参考文献

1. Volkmann RA, et al. PLoS One. 2016 Feb 1;11(2):e0148129.

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