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

Details

Stereochemistry ACHIRAL
Molecular Formula C17H23N3O
Molecular Weight 285.384
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PSN-375,963

SMILES

CCCCC1CCC(CC1)C2=NC(=NO2)C3=CC=NC=C3

InChI

InChIKey=OAVLEYPTWABFLF-UHFFFAOYSA-N
InChI=1S/C17H23N3O/c1-2-3-4-13-5-7-15(8-6-13)17-19-16(20-21-17)14-9-11-18-12-10-14/h9-13,15H,2-8H2,1H3

HIDE SMILES / InChI

Molecular Formula C17H23N3O
Molecular Weight 285.384
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

PSN375963 is agonist of GPR119 receptor. Treatment of mice islet cells with PSN375963 stimulated insuline resistance.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
8.4 µM [EC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct

PubMed

Sample Use Guides

In Vivo Use Guide
In the model of insuline resistance, PSN375963 was administered to mice by intraperitoneal injection in combination with glucose. Dose of 0.1 umol/l/kg did not lead to statistically significant difference in AUC of plasma insulin.
Route of Administration: Intraperitoneal
In Vitro Use Guide
Activity of PSN375963 towards GPR119 was measured in yeast fluorimetric assay and by increase of intracellular cAMP in HEK-OSGPR116 cells expressing GPR119. PSN375963 stimulates GPR119 with EC50 of 8.4 uM.
Substance Class Chemical
Record UNII
C9M28M425E
Record Status Validated (UNII)
Record Version