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VU0469650

Names

[ CAS No. ]:
1443748-47-7

[ Name ]:
VU0469650

[Synonym ]:
3-[(3R)-4-(Adamantan-1-ylcarbonyl)-3-methyl-1-piperazinyl]-2-pyridinecarbonitrile
2-Pyridinecarbonitrile, 3-[(3R)-3-methyl-4-(tricyclo[3.3.1.13,7]dec-1-ylcarbonyl)-1-piperazinyl]-
3-[(3R)-3-Methyl-4-(tricyclo[3.3.1.13,7]dec-1-ylcarbonyl)-1-piperazinyl]-2-pyridinecarbonitrile hydrochloride

Biological Activity

[Description]:

VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> GPCR/G Protein >> mGluR
Research Areas >> Neurological Disease

[Target]

mGluR 1:99 nM (IC50)


[In Vivo]

VU0469650 (male Sprague-Dawley rats, 0.2 mg/kg, IV, once) exhibits moderate to high clearance, a moderate volume of distribution, and a half-life of approximately 1 hour[1]. VU0469650 (male Sprague-Dawley rats, 10 mg/kg, IP, once) shows an excellent selectivity profile and good exposure in both plasma and brain samples[1].

[References]

[1]. Lovell KM, Felts AS, Rodriguez AL, et al. N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg Med Chem Lett. 2013;23(13):3713-3718.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
584.7±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H28N4O

[ Molecular Weight ]:
364.48

[ Flash Point ]:
307.4±30.1 °C

[ Exact Mass ]:
364.226318

[ LogP ]:
3.17

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.624

Related Compounds