Chemical Structure : MPX-004
CAS No.:
1688684-07-2
MPX-004
(MPX004)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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455.91
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Formula
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C17H15ClFN5O3S2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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5-(((3-chloro-4-fluorophenyl)sulfonamido)methyl)-N-((2-methylthiazol-5-yl)methyl)pyrazine-2-carboxamide
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References
1. Volkmann RA, et al. PLoS One. 2016 Feb 1;11(2):e0148129.
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