Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : GNE-9278
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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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.
| M.Wt | 429.539 | |
| Formula | C21H27N5O3S | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
1. Tzu-Ming Wang, et al. Neuropharmacology. 2017 Jul 15;121:204-218.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
