U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C17H24F3N3O3S
Molecular Weight 407.451
Optical Activity NONE
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VELNEPERIT

SMILES

CC(C)(C)S(=O)(=O)N[C@H]1CC[C@@H](CC1)C(=O)NC2=NC=C(C=C2)C(F)(F)F

InChI

InChIKey=WGEWUYACXPEFPO-AULYBMBSSA-N
InChI=1S/C17H24F3N3O3S/c1-16(2,3)27(25,26)23-13-7-4-11(5-8-13)15(24)22-14-9-6-12(10-21-14)17(18,19)20/h6,9-11,13,23H,4-5,7-8H2,1-3H3,(H,21,22,24)/t11-,13-

HIDE SMILES / InChI
Velneperit, also known as S-2367, is a once-daily, oral, centrally acting, small molecule neuropeptide Y (NPY) Y5 receptor antagonist that was discovered by Shionogi Research Laboratories. It was developed for the oral treatment of obesity. Velneperit was in phase II trials, however, development was discontinued.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: Q15761
Gene ID: 4889.0
Gene Symbol: NPY5R
Target Organism: Homo sapiens (Human)
5.3 nM [Ki]
PubMed

PubMed

TitleDatePubMed
New and emerging drug molecules against obesity.
2014 Jan
Current Drug Targets in Obesity Pharmacotherapy - A Review.
2017
Future Pharmacotherapy for Obesity: New Anti-obesity Drugs on the Horizon.
2018 Jun

Sample Use Guides

Obesity: tablet, 4 x 400 mg, taken once daily with morning meal, 54-weeks
Route of Administration: Oral
Velneperit (S-2367) completely displaced the binding of [125I]PYY to membrane homogenates of CHO-K1 cells expressing mouse NPY Y5 receptor, with Ki value of 5.3 ± 0.4 nM. The antagonistic effect of S-2367 for the NPY Y5 receptor was determined using CHO-K1 cells expressing mouse NPY Y5 receptor in a cAMP assay. S-2367 inhibited NPY-mediated decrease in forskolin-induced cAMP formation in a concentration-dependent manner. The IC50 value of S-2367 was 169 ± 29 nM.
Name Type Language
VELNEPERIT
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
Velneperit [WHO-DD]
Common Name English
S-2367
Code English
VELNEPERIT [USAN]
Common Name English
velneperit [INN]
Common Name English
CYCLOHEXANECARBOXAMIDE, 4-(((1,1-DIMETHYLETHYL)SULFONYL)AMINO)-N-(5-(TRIFLUOROMETHYL)- 2-PYRIDINYL)-, TRANS-
Common Name English
TRANS-4-(((1,1-DIMETHYLETHYL)SULFONYL)AMINO)-N-(5-(TRIFLUOROMETHYL)PYRIDIN-2- YL)CYCLOHEXANECARBOXAMIDE
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C29728
Created by admin on Sat Dec 16 17:35:30 GMT 2023 , Edited by admin on Sat Dec 16 17:35:30 GMT 2023
Code System Code Type Description
FDA UNII
09BQ2KJ22J
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INN
9005
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ChEMBL
CHEMBL2016681
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PUBCHEM
20629114
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EPA CompTox
DTXSID20955806
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NCI_THESAURUS
C152850
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CAS
342577-38-2
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USAN
SS-113
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DRUG BANK
DB12889
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SMS_ID
300000034463
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WIKIPEDIA
Velneperit
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