JNJ-5207787 is an antagonist of the neuropeptide Y (NPY) receptor Y₂ that blocks peptide YY binding (IC₅₀ = 100 nM).^1,2 It displays 100-fold selectivity for Y₂ over other NPY receptors and has minimal effect on a panel of 50 receptors, ion channels, and transporters, except for sodium channel 2.¹ JNJ-5207787 is intraperitoneally bioavailable and brain penetrant in rats, occupying maximally 50% of Y₂ receptor binding sites in the hypothalamic area.¹

≥98%

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1.Bonaventure, P.,Nepomuceno, D.,Mazur, C., et al. Characterization of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-ethyl)-piperidin-4yl]acrylamide (JNJ-5207787), a small molecule antagonist of the neuropeptide Y Y2 receptor. J. Pharm. Exp. Ther. 308(3), 1130-1137 (2004).

2.Mittapalli, G.K. and Roberts, E. Ligands of the neuropeptide Y Y2 receptor. Bioorg. Med. Chem. Lett. 24(2), 430-441 (2014).