MedKoo Cat#: 555177 | Name: GNE-9278
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GNE-9278 is a potent and selective NMDA receptor positive allosteric modulator that acts via the transmembrane domain. Mutation of a single residue near the Lurcher motif on GluN1 M3 can convert GNE-9278 modulation from positive to negative, and replacing three AMPAR pre-M1 residues with corresponding NMDAR residues can confer GNE-9278 sensitivity to AMPARs. Modulation by GNE-9278 is state-dependent and significantly alters extracellular domain pharmacology.

Chemical Structure

GNE-9278
GNE-9278
CAS#901230-11-3 (free base)

Theoretical Analysis

MedKoo Cat#: 555177

Name: GNE-9278

CAS#: 901230-11-3 (free base)

Chemical Formula: C21H27N5O3S

Exact Mass: 429.1835

Molecular Weight: 429.54

Elemental Analysis: C, 58.72; H, 6.34; N, 16.30; O, 11.17; S, 7.46

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
25mg USD 950.00 2 Weeks
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Related CAS #
Synonym
GNE-9278; GNE 9278; GNE9278; PAPD5-IN-1
IUPAC/Chemical Name
4-cyclohexyl-N-(5-methyl-7-oxo-2-propyl-4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-6-yl)benzenesulfonamide
InChi Key
OKXCVUICUUOADN-UHFFFAOYSA-N
InChi Code
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)
SMILES Code
O=C1C(NS(C2=CC=C(C3CCCCC3)C=C2)(=O)=O)=C(C)NC4=NC(CCC)=NN41
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Ionotropic glutamate receptors (iGluRs) mediate fast excitatory neurotransmission and are key nervous system drug targets.
Product Data
Biological target:
GNE 9278 is a positive allosteric modulator of NMDA receptors. Potentiates NMDA receptors containing GluN2A, 2B, 2C and 2D subunits (EC50 values are 0.74, 3.07, 0.47 and 0.32 μM in a Ca2+ influx assay, respectively).
In vitro activity:
9278 acts as a PAM rather than as an agonist or co-agonist (Fig. 1D). GNE-9278 increased current in response to pulses of saturating Glu (in the presence of saturating glycine) both by increasing the peak current amplitude and by slowing the deactivation process during Glu washout (Fig. 1E). Reference: Neuropharmacology. 2017 Jul 15;121:204-218. https://pubmed.ncbi.nlm.nih.gov/28457974/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 43.0 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 429.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Wang TM, Brown BM, Deng L, Sellers BD, Lupardus PJ, Wallweber HJA, Gustafson A, Wong E, Volgraf M, Schwarz JB, Hackos DH, Hanson JE. A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain. Neuropharmacology. 2017 Jul 15;121:204-218. doi: 10.1016/j.neuropharm.2017.04.041. Epub 2017 Apr 27. PMID: 28457974.
In vitro protocol:
1. Wang TM, Brown BM, Deng L, Sellers BD, Lupardus PJ, Wallweber HJA, Gustafson A, Wong E, Volgraf M, Schwarz JB, Hackos DH, Hanson JE. A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain. Neuropharmacology. 2017 Jul 15;121:204-218. doi: 10.1016/j.neuropharm.2017.04.041. Epub 2017 Apr 27. PMID: 28457974.
In vivo protocol:
TBD
1: Wang TM, Brown BM, Deng L, Sellers BD, Lupardus PJ, Wallweber HJA, Gustafson A, Wong E, Volgraf M, Schwarz JB, Hackos DH, Hanson JE. A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain. Neuropharmacology. 2017 Jul 15;121:204-218. doi: 10.1016/j.neuropharm.2017.04.041. Epub 2017 Apr 27. PubMed PMID: 28457974.