Description
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.
Product information
CAS Number: 2315311-83-0
Molecular Weight: 429.54
Formula: C21H27N5O3S
Chemical Name: 4-cyclohexyl-N-{5-methyl-7-oxo-2-propyl-3H,7H-[1,2,4]triazolo[1,5-a]pyrimidin-6-yl}benzene-1-sulfonamide
Smiles: CC1N=C2NC(CCC)=NN2C(=O)C=1NS(=O)(=O)C1C=CC(=CC=1)C1CCCCC1
InChiKey: OKXCVUICUUOADN-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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. 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.
Products are for research use only. Not for human use.
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