VU0361737

• CAT Number: I000585
• CAS Number: 1161205-04-4
• Molecular Formula: C13H11ClN2O2
• Molecular Weight: 262.7
• Purity: ≥95%
• Synonyms: N-(4-chloro-3-methoxyphenyl)pyridine-2-carboxamide
• Target: GluR
• Solubility: DMSO: ≥ 43 mg/mL
• Storage: 3 years -20C powder
• IC50: 110 nM (EC50, for rat ), 240 nM (EC50, for human)
• InChI: InChI=1S/C13H11ClN2O2/c1-18-12-8-9(5-6-10(12)14)16-13(17)11-4-2-3-7-15-11/h2-8H,1H3,(H,16,17)
• InChIKey: ARYUXFNGXHNNDM-UHFFFAOYSA-N
• SMILES: O=C(C1=NC=CC=C1)NC2=CC=C(Cl)C(OC)=C2

VU0361737(CAT: I000585) plays a pivotal role in the field of neuropharmacology and receptor modulation research. Operating as a selective positive allosteric modulator (PAM), it targets the metabotropic glutamate receptor subtype mGlu4. With an EC50 of 240 nM and 110 nM at human and rat receptors respectively, VU0361737 offers potential in fine-tuning mGlu4 receptor activity. Its selective action, particularly with weak activity at mGlu5 and mGlu8 receptors and inactivity at mGlu1, mGlu2, mGlu3, mGlu6, and mGlu7 receptors, highlights its specificity for mGlu4.

Reference

[1]. Jantas D, et al. Neuroprotective effects of metabotropic glutamate receptor group II and III activators against MPP(+)-induced cell death in human neuroblastoma SH-SY5Y cells: the impact of cell differentiation state. Neuropharmacology. 2014 Aug;83:36-53.
[2]. Jantas D, et al. Neuroprotective effects of mGluR II and III activators against staurosporine- and doxorubicin-induced cellular injury in SH-SY5Y cells: New evidence for a mechanism involving inhibition of AIF translocation. Neurochem Int. 2015 Sep;88:124-37.
[3]. Engers DW, et al. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J Med Chem. 2009 Jul 23;52(14):4115-8.
[4]. Engers DW, et al. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. J Med Chem. 2011 Feb 24;54(4):1106-10.