GNE 5729

Names

[ CAS No. ]:
2026635-66-3

[ Name ]:
GNE 5729

[Synonym ]:
MFCD30829916
(1R,2R)-2-(7-Chloro-2-{[5-chloro-3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl}-4-oxo-4H-pyrido[1,2-a]pyrimidin-6-yl)cyclopropanecarbonitrile
Cyclopropanecarbonitrile, 2-[7-chloro-2-[[5-chloro-3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]-4-oxo-4H-pyrido[1,2-a]pyrimidin-6-yl]-, (1R,2R)-

Biological Activity

[Description]:

GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR
Signaling Pathways >> Neuronal Signaling >> iGluR
Research Areas >> Neurological Disease

[Target]

EC50: 37 nM (GluN2A), 4.7 μM (GluN2C), 9.5 μM (GluN2D)[1]


[In Vitro]

GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively[1].

[References]

[1]. Villemure E, et al. GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile. ACS Med Chem Lett. 2016 Oct 31;8(1):84-89.


[Related Small Molecules]

(+)-MK 801 Maleate | CNQX | N-Methyl-D-aspartic acid | ifenprodil tartrate | D-AP5(mM/ml) | DNQX | Ro 25-6981 maleate | Flupirtine maleate | Mibampator | CX546 | Naspm | Talampanel | Centrophenoxine hydrochloride | 24-Hydroxycholesterol

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Boiling Point ]:
527.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C17H10Cl2F3N5O

[ Molecular Weight ]:
428.195

[ Flash Point ]:
272.9±32.9 °C

[ Exact Mass ]:
427.021454

[ LogP ]:
2.73

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.702

Related Compounds