JNJ-5207787 

JNJ-5207787 is a nonpeptidic, selective and penetrate the blood-brain barrier neuropeptide Y Y₂ receptor (Y₂) antagonist. JNJ-5207787 inhibits the binding of peptide YY (PYY) with pIC₅₀s of 7.0 and 7.1 for human Y₂ receptor and rat Y₂ receptor, respectively. JNJ-5207787 is >100-fold selective versus human Y₁, Y₄, and Y₅ receptors^[1].

JNJ-5207787 (0.01, 0.1, 1, 10 μM) has antagonistic properties and inhibits the PYY-stimulated [³⁵S]GTPγS binding to basal level with a p IC₅₀ corr of 7.20^[1].
JNJ-5207787 (10 μM; 15 min) inhibits [¹²⁵I]PYY labeling in lateral septum, cerebellum, ventral tegmental area, substantia nigra, hippocampus, septum, amygdala, and hypothalamus^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ-5207787 (i.p.; 30 mg/kg) penetrates into the brain (C_max=1351 ng/ml at 30 min) and occupies Y₂ receptor binding sites^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

510.67

C₃₂H₃₈N₄O₂

683746-68-1

Solid

White to off-white

N#CC1=CC=CC(/C=C/C(N(C2CCN(CCC3CCCC3)CC2)C4=CC=C(CCN5C(C)=O)C5=C4)=O)=C1

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Bonaventure P, 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 YY2 receptor. J Pharmacol Exp Ther. 2004  [Content Brief]