All Photos(1)
Synonym(s):
4-Cyclohexyl-N-(7-hydroxy-5-methyl-2-propyl[1,2,4]triazolo[1,5-a]pyrimidin-6-yl)-benzenesulfonamide, GNE 9278, GNE9278
Empirical Formula (Hill Notation):
C21H27N5O3S
Recommended Products
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
CC1=NC2=NC(CCC)=NN2C(O)=C1NS(C3=CC=C(C4CCCCC4)C=C3)(=O)=O
Biochem/physiol Actions
GNE-9278 is a selective NMDAR, but not AMPAR, positive allosteric modulator (PAM fold enhancement Emax/EC50 = 5.5/0.74 μM/2A, 8.4/3.07 μM/2B,10.2/0.47 μM/2C, 7.9/0.32 μM/2D of gly EC50 (50 μM)-induced Ca++ influx in HEK293 co-expressing GluN1 & respective GluN2 subunit; Emax/EC50 = 4.6/3.2 μM/2A,12.4/15.7 μM/2B, 9.1/6.6 μM/2C, 14.9/6.7 μM/2D of 100 μM Glu-induced current in the presence of 50 μM 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.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
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Tzu-Ming Wang et al.
Neuropharmacology, 121, 204-218 (2017-05-02)
Ionotropic glutamate receptors (iGluRs) mediate fast excitatory neurotransmission and are key nervous system drug targets. While diverse pharmacological tools have yielded insight into iGluR extracellular domain function, less is known about molecular mechanisms underlying the ion conduction gating process within
Erica S Burnell et al.
Journal of medicinal chemistry, 62(1), 3-23 (2018-02-16)
Excitatory activity in the CNS is predominately mediated by l-glutamate through several families of l-glutamate neurotransmitter receptors. Of these, the N-methyl-d-aspartate receptor (NMDAR) family has many critical roles in CNS function and in various neuropathological and psychiatric conditions. Until recently
Ioana Neagoe et al.
Stem cell research, 28, 105-114 (2018-02-18)
Abnormal signaling pathways mediated by N-methyl-d-aspartate receptors (NMDARs) have been implicated in the pathogenesis of various CNS disorders and have been long considered as promising points of therapeutic intervention. However, few efforts have been previously described concerning evaluation of therapeutic
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