GNE-9278 | NMDAR PAM | Probechem Biochemicals

Chemical Structure : GNE-9278

GNE-9278 (GNE9278)

Catalog No.: PC-49066Not For Human Use, Lab Use Only.

GNE-9278 is a potent NMDAR positive allosteric modulator (PAM) that acts at the GluN1 transmembrane domain (TMD), robustly potentiates GluN2A, 2B, 2C and 2D-containing NMDARs in calcium influx assays from HEK cell lines with EC50 values of 0.74, 3.07, 0.47, and 0.32 μM, respectively, and maximum fold potentiation of 5.5, 8.4, 10.2 and 7.9, respectively.

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Biological Activity

GNE-9278 is a potent NMDAR positive allosteric modulator (PAM) that acts at the GluN1 transmembrane domain (TMD), robustly potentiates GluN2A, 2B, 2C and 2D-containing NMDARs in calcium influx assays from HEK cell lines with EC50 values of 0.74, 3.07, 0.47, and 0.32 μM, respectively, and maximum fold potentiation of 5.5, 8.4, 10.2 and 7.9, respectively.
GNE-9278 is highly selective for NMDARs vs. AMPARs, with no appreciable activity in AMPAR calcium influx assays.
GNE-9278 demonstrates robust potentiation of GluN2A, 2B, 2C and 2D-containing NMDARs in electrophysiology experiments in oocytes with EC50 values of 3.2, 15.7, 6.6 and 6.7 μM, respectively, and maximum fold potentiation of 4.6, 12.4, 9.1 and 14.9, respectively.
Modulation by GNE-9278 is state-dependent and significantly alters extracellular domain pharmacology.

Physicochemical Properties

M.Wt	429.539
Formula	C21H27N5O3S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-cyclohexyl-N-(5-methyl-7-oxo-2-propyl-4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-6-yl)benzenesulfonamide

References

1. Tzu-Ming Wang, et al. Neuropharmacology. 2017 Jul 15;121:204-218.

GNE-9278 (GNE9278)

Biological Activity

Physicochemical Properties

References

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