JNJ-5207787 - CAS# 683746-68-1


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M16238-C Contact sales@xcessbio.com for quotation $100

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.

Product information

CAS Number: 683746-68-1

Molecular Weight: 510.67

Formula: C32H38N4O2

Chemical Name: (2E)-N-(1-acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)piperidin-4-yl]prop-2-enamide

Smiles: CC(=O)N1CCC2=CC=C(C=C12)N(C1CCN(CCC2CCCC2)CC1)C(=O)/C=C/C1=CC(=CC=C1)C#N

InChiKey: DSEJCLDJIFTPPH-FMIVXFBMSA-N

InChi: 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+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. JNJ-5207787 (10 μM; 15 min) inhibits [125I]PYY labeling in lateral septum, cerebellum, ventral tegmental area, substantia nigra, hippocampus, septum, amygdala, and hypothalamus.

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.

Products are for research use only. Not for human use.

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