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Details

Stereochemistry ACHIRAL
Molecular Formula C26H29N5O2S
Molecular Weight 475.606
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CGP-71683A FREE BASE

SMILES

NC1=C2C=CC=CC2=NC(NC[C@H]3CC[C@H](CNS(=O)(=O)C4=C5C=CC=CC5=CC=C4)CC3)=N1

InChI

InChIKey=UULIGRNKXHCLQN-WGSAOQKQSA-N
InChI=1S/C26H29N5O2S/c27-25-22-9-3-4-10-23(22)30-26(31-25)28-16-18-12-14-19(15-13-18)17-29-34(32,33)24-11-5-7-20-6-1-2-8-21(20)24/h1-11,18-19,29H,12-17H2,(H3,27,28,30,31)/t18-,19-

HIDE SMILES / InChI
Molecular Formula C26H29N5O2S
Molecular Weight 475.606
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800010609

CGP-71683A is a non-peptidic neuropeptide Y (NPY) Y5 receptor antagonist that was under development by Novartis. CGP-71683A is an extremely selective, non-peptide NPY Y5 receptor antagonist, displaying > 1000-fold selectivity over Y1, Y2 and Y4 receptors; IC50 values are 1.4, 2765, 7187 and 5637 nM at cloned rat Y5, Y1, Y2 and Y4 receptors respectively. CGP-71683A potently inhibits NPY-induced food intake following i.p. administration in diabetic, free-feeding and fasted rats.

CNS Activity

Originator

Novartis
173
Curator's Comment: # Novartis

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 1.3 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Preclinical
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
Development and characterization of a highly selective neuropeptide Y Y5 receptor agonist radioligand: [125I][hPP1-17, Ala31, Aib32]NPY.
2003 Aug
Patents

Patents

US8148395
2
US8173674
2
US8222240
2

Sample Use Guides

In Vivo Use Guide
Rats: CGP-71683A (1-10 mg/kg, i.p.) dose-dependently decreased nocturnal and fasting-induced food intake.
Route of Administration: Intraperitoneal
In Vitro Use Guide
1 umol/L CGP-71683A completely blocked cell growth of MCF-7 cells
Substance Class Chemical
Created
by admin
on Sat Dec 16 09:24:13 GMT 2023
Edited
by admin
on Sat Dec 16 09:24:13 GMT 2023
Record UNII
E4901JA9JD
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CGP-71683A FREE BASE
Common Name English
1-NAPHTHALENESULFONAMIDE, N-((4-(((4-AMINO-2-QUINAZOLINYL)AMINO)METHYL)CYCLOHEXYL)METHYL)-, TRANS-
Systematic Name English
1-NAPHTHALENESULFONAMIDE, N-((TRANS-4-(((4-AMINO-2-QUINAZOLINYL)AMINO)METHYL)CYCLOHEXYL)METHYL)-
Systematic Name English
Code System Code Type Description
PUBCHEM
5312114
Created by admin on Sat Dec 16 09:24:13 GMT 2023 , Edited by admin on Sat Dec 16 09:24:13 GMT 2023
PRIMARY
FDA UNII
E4901JA9JD
Created by admin on Sat Dec 16 09:24:13 GMT 2023 , Edited by admin on Sat Dec 16 09:24:13 GMT 2023
PRIMARY
CAS
192321-23-6
Created by admin on Sat Dec 16 09:24:13 GMT 2023 , Edited by admin on Sat Dec 16 09:24:13 GMT 2023
PRIMARY
Related Record Type Details
Structure of CGP-71683A FREE BASE
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