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VU 0364439

Names

[ CAS No. ]:
1246086-78-1

[ Name ]:
VU 0364439

[Synonym ]:
cc-720
CS-1000
2-Pyridinecarboxamide, N-[3-chloro-4-[[(2-chlorophenyl)amino]sulfonyl]phenyl]-
N-{3-Chloro-4-[(2-chlorophenyl)sulfamoyl]phenyl}-2-pyridinecarboxamide
2-Pyridinecarboxamide (N-[3-chloro-4-[[(2-chlorophenyl)amino]sulfonyl]phenyl]
VU0364439
VU 0364439

Biological Activity

[Description]:

VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.IC50 Value: 19.8 nM(EC50)Target: mGluRin vitro:in vivo: VU 0364439 possess less than ideal PK properties preventing their use as in vivo tools. It shows better stability in HLM (63% remaining) than RLM (2% remaining).

[Related Catalog]:

Research Areas >> Neurological Disease

[References]

[1]. Hong, Sang-Phyo; Liu, Kevin G.; Ma, Gil et al. Tricyclic Thiazolopyrazole Derivatives as Metabotropic Glutamate Receptor 4 Positive Allosteric Modulators. Journal of Medicinal Chemistry (2011), 54(14), 5070-5081.

[2]. Engers, Darren W.; Gentry, Patrick R.; Williams, Richard et al. Synthesis and SAR of novel 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorganic & Medicinal Chem

[3]. AJ Robichaud et al. Recent Progress on the Identification of Metabotropic Glutamate 4 Receptor Ligands and Their Potential Utility as CNS Therapeutics. ACS Chem. Neurosci. 2011, 2(8), 433-449.


[Related Small Molecules]

mavoglurant | L-Glutamine | CTEP (RO4956371) | LY 354740 | L-(+)Sodium glutamate | ADX-88178 | MPEP (Hydrochloride) | FITM | (S)-MCPG | Basimglurant | LY341495 | Dipraglurant | JNJ-40411813 | LY404039 | JNJ 16259685

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C18H13Cl2N3O3S

[ Molecular Weight ]:
422.285

[ Exact Mass ]:
421.005463

[ PSA ]:
100.03000

[ LogP ]:
3.82

[ Index of Refraction ]:
1.686

[ Storage condition ]:
-20°C

Related Compounds