MPX-004 

MPX-004 is a potent GluN2A antagonist. MPX-004 inhibits GluN2A-containing NMDA receptors expressed in HEK cells with an IC₅₀ of 79 nM. MPX-004 has no inhibitory effect on GluN2B or GluN2D receptor-mediated responses. MPX-004 has the potential for neuropsychiatric and developmental disorders research^[1].

MPX-004 inhibits NMDA receptor-mediated currents in Xenopus oocytes expressing human GluN1 + GluN2A with an IC₅₀ of 198 nM. At 10 μM, MPX-004 only weakly (up to 8%) inhibits currents in oocytes expressing GluN2B, C, or D receptors or in control oocytes^[1].
MPX-004 (100 nM-30 μM; 0-50 min) causes a concentration-dependent reduction in NMDA receptor-mediated fEPSPs in region CA1 in response to Schaffer collateral stimulation in hippocampal slices prepared from brains of 3- to 4-week old rats^[1].
MPX-004 (1 μM) inhibits 5-HT_1B antagonist binding by 35%, 5-HT_2A agonist binding by 31% and EP4 agonist binding by 27%. MPX-004 (50 μM) has no effect on AMPA receptor-mediated synaptic currents of pyramidal neurons in slices from mouse visual cortex- currents^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

455.91

C₁₇H₁₅ClFN₅O₃S₂

1688684-07-2

Solid

White to light yellow

O=C(C1=NC=C(CNS(=O)(C2=CC=C(C(Cl)=C2)F)=O)N=C1)NCC3=CN=C(C)S3

Room temperature in continental US; may vary elsewhere.

• [1]. Robert A Volkmann, et al. MPX-004 and MPX-007: New Pharmacological Tools to Study the Physiology of NMDA Receptors Containing the GluN2A Subunit. PLoS One. 2016 Feb 1;11(2):e0148129.  [Content Brief]