PeptideDB

MPX-004

CAS: 1688684-07-2 F: C17H15ClFN5O3S2 W: 455.91

MPX-004 is a potent GluN2A antagonist. MPX-004 inhibits GluN2A-containing NMDA receptors expressed in HEK cells with an
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Bioactivity 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].
Invitro MPX-004 抑制表达人 GluN1+GluN2A 的 Xenopus 卵母细胞中 NMDA 受体介导的电流,IC50 为 198 nM。在 10 μM 时,MPX-004 仅微弱地抑制表达 GluN2B、C 或 D 受体的卵母细胞或对照卵母细胞中的电流 (约8%)[1]。 MPX-004 (100 nM-30 μM; 0-50 分钟) 在 3 至 4 周龄大鼠大脑制备的海马切片导致 CA1 区 NMDA 受体介导的 fEPSP 浓度依赖性降低,以响应 Schaffer 侧支刺激[1]。 MPX-004 (1 μM) 抑制 5-HT1B 拮抗剂结合 (35%),5-HT2A 激动剂结合 (31%) 和 EP4 激动剂结合 (27%)。MPX-004 (50 μM) 对小鼠视觉皮层电流切片中锥体神经元的 AMPA 受体介导的突触电流没有影响[1]。
Name MPX-004
CAS 1688684-07-2
Formula C17H15ClFN5O3S2
Molar Mass 455.91
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [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.