2. GPCR/G Protein Neuronal Signaling
  3. Neuropeptide Y Receptor
  4. 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.

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JNJ-5207787 Chemical Structure

JNJ-5207787 Chemical Structure

CAS No. : 683746-68-1

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JNJ-5207787 Related Antibodies

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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].

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

JNJ-5207787 Related Antibodies
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].

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

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.
Appearance

Solid

Color

White to off-white

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
Solvent & Solubility
In Vitro: 

DMSO : ≥ 5 mg/mL (9.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9582 mL 9.7911 mL 19.5821 mL
5 mM 0.3916 mL 1.9582 mL 3.9164 mL
View the Complete Stock Solution Preparation Table

* 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.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9582 mL 9.7911 mL 19.5821 mL 48.9553 mL
5 mM 0.3916 mL 1.9582 mL 3.9164 mL 9.7911 mL
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JNJ-5207787 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-5207787683746-68-1JNJ5207787JNJ 5207787Neuropeptide Y ReceptorNPY receptornonpeptidicselectiveblood-brainbarrierY2peptideYYPYYY1Y4Y5,Inhibitorinhibitorinhibit

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