Bioactivity | GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity[1]. | ||||||||||||
Target | NMDAR | ||||||||||||
Invitro | GNE-9278 (50 μM) slows deactivation with multiple agonists (D-Glu, L-Glu and L-CCG-IV) and enhances the potency of both Glu and Gly[1].GNE-9278 robustly potentiates GluN2A, 2B, 2C and 2D-containing NMDARs as measured by calcium influx assays from HEK cell lines with EC50s of 0.74, 3.07, 0.47, and 0.32 μM, respectively[1]. | ||||||||||||
Name | GNE-9278 | ||||||||||||
CAS | 2315311-83-0 | ||||||||||||
Formula | C21H27N5O3S | ||||||||||||
Molar Mass | 429.54 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Wang TM, et, al. A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain. Neuropharmacology. . 2017 Jul 15; 121: 204-218. |