1. GPCR/G Protein
    Neuronal Signaling
  2. Neuropeptide Y Receptor
  3. JNJ-5207787

JNJ-5207787 

Cat. No.: HY-107732 Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

JNJ-5207787 Chemical Structure

JNJ-5207787 Chemical Structure

CAS No. : 683746-68-1

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Description

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].

IC50 & Target[1]

human Y2 receptor

7.0 (pIC50)

rat Y2 receptor

7.1 (pIC50)

In Vitro

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].

In Vivo

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

Animal Model: Sixteen female Sprague-Dawley Rats (approximately 300 g of body weight)[1]
Dosage: 30 mg/kg
Administration: IP
Result: Penetrated into the brain (Cmax=1351 ng/ml at 30 min) and occupied Y2 receptor binding sites.
Molecular Weight

510.67

Formula

C₃₂H₃₈N₄O₂

CAS No.

683746-68-1

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >98.0%

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Keywords:

JNJ-5207787JNJ5207787JNJ 5207787Neuropeptide Y ReceptorNPY receptornonpeptidicselectiveblood-brainbarrierY2peptideYYPYYY1Y4Y5,Inhibitorinhibitorinhibit

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JNJ-5207787
Cat. No.:
HY-107732
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