VU 0364439

• CAT Number: I000976
• CAS Number: 1246086-78-1
• Molecular Formula: C18H13Cl2N3O3S
• Molecular Weight: 422.3
• Purity: ≥95%
• Synonyms: N-[3-chloro-4-[(2-chlorophenyl)sulfamoyl]phenyl]pyridine-2-carboxamide
• Target: GluR
• 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

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).

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.