VU 0364439

• CAT Number: I000976
• CAS Number: 1246086-78-1
• Molecular Formula: C18H13Cl2N3O3S
• Molecular Weight: 422.30
• Purity: ≥95%
• Synonyms: N-[3-chloro-4-[(2-chlorophenyl)sulfamoyl]phenyl]pyridine-2-carboxamide
• Target: Neuronal Signaling
• Solubility: 10 mM in DMSO
• Storage: 3 years -20C powder
• IC50: 19.8 nM(EC50)
• InChI: InChI=1S/C18H13Cl2N3O3S/c19-13-5-1-2-6-15(13)23-27(25,26)17-9-8-12(11-14(17)20)22-18(24)16-7-3-4-10-21-16/h1-11,23H,(H,22,24)
• InChIKey: IXHCGJXBIHHIEF-UHFFFAOYSA-N
• SMILES: O=C(C1=NC=CC=C1)NC2=CC=C(S(NC3=CC=CC=C3Cl)(=O)=O)C(Cl)=C2

VU0364439 (Cat No.: I000976) is a selective, brain-penetrant positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 5 (mGlu5). It enhances mGlu5 receptor activity without directly activating it, making it a promising tool for studying neurological disorders like schizophrenia and cognitive deficits. VU0364439 has shown efficacy in preclinical models, improving synaptic plasticity and cognitive function. Its selectivity for mGlu5 reduces off-target effects, making it valuable for neuroscience research and potential therapeutic applications in psychiatric and neurodegenerative diseases.

Reference

[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 Chemistry Letters (2010), 20(17), 5175-5178.
[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.