1246086-78-1

1246086-78-1 structure

Name: VU 0364439
Chemical Name: N-[3-chloro-4-[(2-chlorophenyl)sulfamoyl]phenyl]pyridine-2-carboxamide
CAS Number: 1246086-78-1
Molecular Formula: C₁₈H₁₃Cl₂N₃O₃S
Molecular Weight: 422.285
Catalog: Biochemical Inhibitor Neuronal Signaling GluR regulator
Create Date: 2016-06-16 04:43:36
Modify Date: 2024-01-02 18:05:42
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).

Name	N-[3-chloro-4-[(2-chlorophenyl)sulfamoyl]phenyl]pyridine-2-carboxamide
Synonyms	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

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.