Synonyms: 4-Cyclohexyl-N-(7-hydroxy-5-methyl-2-propyl[1,2,4]triazolo[1,5-a]pyrimidin-6-yl)-benzenesulfonamide; GNE 9278; GNE9278
Molecular Formula: C21H27N5O3S
Molecular Weight: 429.54
Linear Structural Formula: C21H27N5O3S
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: GNE-9278 is a selective NMDAR, but not AMPAR, positive allosteric modulator (PAM fold enhancement Emax/EC50 = 5.5/0.74 muM/2A, 8.4/3.07 muM/2B,10.2/0.47 muM/2C, 7.9/0.32 muM/2D of gly EC50 (50 muM)-induced Ca++ influx in HEK293 co-expressing GluN1 & respective GluN2 subunit; Emax/EC50 = 4.6/3.2 muM/2A,12.4/15.7 muM/2B, 9.1/6.6 muM/2C, 14.9/6.7 muM/2D of 100 muM Glu-induced current in the presence of 50 muM gly using respective GluN1/GluN2 oocytes). GNE-9278 targets transmembrane domain (TMD) extracellular surface of agonist-bound NMDARs, stabilizing NMDARs in an activated state by slowing L-L-glu & gly off-rate.