Methoxy-PEPy

• CAT Number: I003920
• CAS Number: 524924-76-3
• Molecular Formula: C13H10N2O
• Molecular Weight: 210.236
• Purity: ≥95%
• Target: mGlu5R inhibitor
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 1 nM [1]
• IUPAC Name: 3-methoxy-5-(2-pyridin-2-ylethynyl)pyridine
• InChI: InChI=1S/C13H10N2O/c1-16-13-8-11(9-14-10-13)5-6-12-4-2-3-7-15-12/h2-4,7-10H,1H3
• InChIKey: VRTFKUFTEWQHDD-UHFFFAOYSA-N
• SMILES: COC1=CN=CC(=C1)C#CC2=CC=CC=N2

Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM.IC50 value: 1 nM [1]Target: mGlu5R inhibitorAdministration of [3H]methoxy-PEPy (50 microCi/kg i.v.) to mGlu5 receptor-deficient mice revealed binding at background levels in forebrain, whereas wild-type mice exhibited 14-fold higher binding in forebrain relative to cerebellum [2]. The calcium transients stimulated by these agonists were potently inhibited by reference allosteric mGlu5 antagonists – 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and 3-methoxy-5-(pyridine-2-ylethynyl)pyridine (methoxy-PEPy) (IC(50) ranges: 0.8-66 nM) [3].

Reference

[1]. Cosford ND, et al. [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. Bioorg Med Chem Lett. 2003 Feb 10;13(3):351-4.
[2]. Anderson JJ, et al. In vivo receptor occupancy of mGlu5 receptor antagonists using the novel radioligand [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine). Eur J Pharmacol. 2003 Jul 18;473(1):35-40.
[3]. Salisbury BG, et al. Inducible expression and pharmacological characterization of the mouse metabotropic glutamate 5b receptor. Eur J Pharmacol. 2008 Jan 28;579(1-3):34-9.