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1237541-73-9

1237541-73-9 Structure

1237541-73-9 Structure
IdentificationBack Directory
[Name]

NAB-14
[CAS]

1237541-73-9
[Synonyms]

NAB-14
4-((1H-Indol-7-yl)carbamoyl)phenyldiethylcarbamate
Carbamic acid, N,N-diethyl-, 4-[(1H-indol-7-ylamino)carbonyl]phenyl ester
[Molecular Formula]

C20H21N3O3
[MOL File]

1237541-73-9.mol
[Molecular Weight]

351.4
Chemical PropertiesBack Directory
[Boiling point ]

489.5±41.0 °C(Predicted)
[density ]

1.277±0.06 g/cm3(Predicted)
[storage temp. ]

2-8°C
[solubility ]

DMSO: 2mg/mL, clear
[form ]

Solid
[pka]

14.14±0.43(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier[1].
[Biological Activity]

NAB-14 is a negative allosteric modulator (NAM) selective for GluN2C/2D-containing NMDA glutamate receptors. NAB-14 was >800-fold selective for recombinant GluN2C/GluN2D over GluN2A/GluN2B in Xenopus oocytes and exhibited an IC50 value of 580 nM at recombinant GluN1/GluN2D receptors.
[in vivo]

NAB-14 (20 mg/kg; p.o.) shows high systemic exposure with peak brain free of 3.2 and 3.8 nM for mouse and rat, respectively[1].

Animal Model:Mice and rats[1]
Dosage:20 mg/kg
Administration:P.o.
Result:Showed high systemic exposure with peak brain free of 3.2 and 3.8 nM for mouse and rat, respectively.
[References]

[1] Swanger SA, et al. A Novel Negative Allosteric Modulator Selective for GluN2C/2D-Containing NMDA Receptors Inhibits Synaptic Transmission in Hippocampal Interneurons. ACS Chem Neurosci. 2018 Feb 21;9(2):306-319. DOI:10.1021/acschemneuro.7b00329
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