ChemicalBook > CAS DataBase List > (2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide

(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide

Product Name
(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide
CAS No.
683746-68-1
Chemical Name
(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide
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)-
CBNumber
CB32518575
Molecular Formula
C32H38N4O2
Formula Weight
511
MOL File
683746-68-1.mol
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(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide Property

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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
13947
Product name
JNJ-5207787
Purity
≥98%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
13947
Product name
JNJ-5207787
Purity
≥98%
Packaging
5mg
Price
$163
Updated
2024/03/01
Cayman Chemical
Product number
13947
Product name
JNJ-5207787
Purity
≥98%
Packaging
10mg
Price
$296
Updated
2024/03/01
Cayman Chemical
Product number
13947
Product name
JNJ-5207787
Purity
≥98%
Packaging
50mg
Price
$1184
Updated
2024/03/01
Tocris
Product number
4018
Product name
JNJ5207787
Purity
≥98%(HPLC)
Packaging
10
Price
$293
Updated
2021/12/16
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(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide Chemical Properties,Usage,Production

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)

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

(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide Preparation Products And Raw materials

Raw materials

Preparation Products

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(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide Suppliers

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3B Pharmachem (Wuhan) International Co.,Ltd.
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683746-68-1, (2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamideRelated Search:


  • (2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide
  • JNJ 5207787
  • trans-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)piperidin-4-yl]acrylamide
  • (E)-N-(1-acetyl-2,3-dihydroindol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)piperidin-4-yl]prop-2-enamide
  • 2-Propenamide, N-(1-acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-, (2E)-
  • 683746-68-1
  • C32H38N4O2