An antagonist of NPY receptor Y2
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JNJ-5207787

Item No. 13947

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-N-(1-acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide
CAS Number
683746-68-1
Molecular Formula
C32H38N4O2
Formula Weight
510.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 5 mg/ml (gentle warming)Ethanol: 5 mg/ml (gentle warming)
λmax
219, 262 nm
SMILES
O=C(/C=C/C1=CC=CC(C#N)=C1)N(C2=CC=C(CCN3C(C)=O)C3=C2)C4CCN(CCC5CCCC5)CC4
InChi Code
InChI=1S/C32H38N4O2/c1-24(37)35-20-14-28-10-11-30(22-31(28)35)36(32(38)12-9-26-7-4-8-27(21-26)23-33)29-15-18-34(19-16-29)17-13-25-5-2-3-6-25/h4,7-12,21-22,25,29H,2-3,5-6,13-20H2,1H3/b12-9+
InChi Key
DSEJCLDJIFTPPH-FMIVXFBMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $58

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    5 mg

    $215

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    10 mg

    $372

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    Product Description

    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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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).