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Details

Stereochemistry ACHIRAL
Molecular Formula C18H24N4O4
Molecular Weight 360.4076
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PSN-632408

SMILES

CC(C)(C)OC(=O)N1CCC(CC1)OCC2=NC(=NO2)C3=CC=NC=C3

InChI

InChIKey=LHZWKWCEAXQUMX-UHFFFAOYSA-N
InChI=1S/C18H24N4O4/c1-18(2,3)25-17(23)22-10-6-14(7-11-22)24-12-15-20-16(21-26-15)13-4-8-19-9-5-13/h4-5,8-9,14H,6-7,10-12H2,1-3H3

HIDE SMILES / InChI

Molecular Formula C18H24N4O4
Molecular Weight 360.4076
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

PSN632408 is an optimized agonist of GPR119 receptors. Systemic administration of PSN632408 suppresses food intake, reduces weight gain and white adipose tissue deposition in rats. PSN632408 treatment improved the function and/or mass of β-cells, significantly increased both human α- and β-cell areas in islet grafts and stimulated α- and β-cell replication. PSN632408 may be useful as a therapeutic agent for the treatment of obesity, diabetes and related metabolic disorders.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
5.6 µM [EC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown

PubMed

Sample Use Guides

In Vivo Use Guide
100 mg/kg was administered daily for 14 days
Route of Administration: Oral
In Vitro Use Guide
The HEK-OSGPR116 cell line was used to investigate the effect of GPR119 agonists on intracellular levels of cyclic AMP (cAMP). Treatment with PSN632408 produced concentration-dependent increases in cAMP level with mean EC50 values of 1.9 uM.
Substance Class Chemical
Record UNII
V4434XWK2P
Record Status Validated (UNII)
Record Version