For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I045775 |
| CAS Number | 2315311-83-0 |
| Synonyms | 4-cyclohexyl-N-(5-methyl-7-oxo-2-propyl-1H-[1,2,4]triazolo[1,5-a]pyrimidin-6-yl)benzenesulfonamide |
| Molecular Formula | C21H27N5O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C21H27N5O3S/c1-3-7-18-23-21-22-14(2)19(20(27)26(21)24-18)25-30(28,29)17-12-10-16(11-13-17)15-8-5-4-6-9-15/h10-13,15,25H,3-9H2,1-2H3,(H,22,23,24) |
| InChIKey | OKXCVUICUUOADN-UHFFFAOYSA-N |
| SMILES | CCCC1=NC2=NC(=C(C(=O)N2N1)NS(=O)(=O)C3=CC=C(C=C3)C4CCCCC4)C |
| 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. |
