| Identification | Back Directory | [Name]
(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide | [CAS]
683746-68-1 | [Synonyms]
JNJ 5207787
(E)-N-(1-acetyl-2,3-dihydroindol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)piperidin-4-yl]prop-2-enamide
trans-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)piperidin-4-yl]acrylamide
(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide
2-Propenamide, N-(1-acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-, (2E)- | [Molecular Formula]
C32H38N4O2 | [MDL Number]
MFCD19690929 | [MOL File]
683746-68-1.mol | [Molecular Weight]
511 |
| Chemical Properties | Back Directory | [density ]
1.22 | [storage temp. ]
Store at RT | [solubility ]
Soluble to 10 mM in DMSO with gentle warming and to 10 mM in ethanol with gentle warming | [form ]
Powder | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
JNJ-5207787 is an antagonist of the neuropeptide Y (NPY) receptor Y2 that blocks peptide YY binding (IC50 = 100 nM). 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. JNJ-5207787 is intraperitoneally bioavailable and brain penetrant in rats, occupying maximally 50% of Y2 receptor binding sites in the hypothalamic area. | [Uses]
JNJ 5207787 is a small molecule antagonist of the neuropeptide Y Y2 receptor. | [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.
|
| [IC 50]
human Y2 receptor: 7.0 (pIC50); rat Y2 receptor: 7.1 (pIC50) | [storage]
Store at RT | [References]
[1] PASCAL BONAVENTURE. 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]. Journal of Pharmacology and Experimental Therapeutics, 2004, 308 3: 1130-1137. DOI: 10.1124/jpet.103.060459
[2] G. MITTAPALLI E R. Ligands of the Neuropeptide Y Y2 Receptor[J]. ChemInform, 2014, 46 1. DOI: 10.1002/chin.201410270 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
|