CGP-71683A FREE BASE

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 Search

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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9854049
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

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Neuropeptide Y receptor type 5 5 Target ID: CHEMBL4561 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10737674 \| https://www.ncbi.nlm.nih.gov/pubmed/15863317 \| https://www.ncbi.nlm.nih.gov/pubmed/14677152 \| https://www.ncbi.nlm.nih.gov/pubmed/11244462	Antagonist 2778		1.3 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Obesity 203 Sources: http://adisinsight.springer.com/drugs/800010609 https://www.ncbi.nlm.nih.gov/pubmed/11239922 https://www.ncbi.nlm.nih.gov/pubmed/10704716	Primary		Preclinical	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed

Patents

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


					E4901JA9JD

CGP-71683A FREE BASE

ACTIVE MOIETY

Details

SMILES

InChI

DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/9854049Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800010609

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

PubMed

Patents

Sample Use Guides

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9854049
Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800010609