PSN632408

Names

[ Name ]:
PSN632408

[Synonym ]:
2-Methyl-2-propanyl 4-{[3-(4-pyridinyl)-1,2,4-oxadiazol-5-yl]methoxy}-1-piperidinecarboxylate
PSN-632,408
1-Piperidinecarboxylic acid, 4-[[3-(4-pyridinyl)-1,2,4-oxadiazol-5-yl]methoxy]-, 1,1-dimethylethyl ester
PSN632408

Biological Activity

[Description]:

PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 uM, respectively.IC50 value: 5.6/7.9 uM ( recombinant mouse/ human GPR119) [1]Target: GPR119 agonistSystemic administration of PSN632408 (30 mg/kgintraperitoneally) suppresses food intake, reduces weight gain, and white adipose tissue deposition in rats. GPR119 (previously designated SNORF25) is an orphan G protein-coupled receptor expressed predominantly in the pancreas and gastrointestinal tract in humans and in the brain, pancreas, and gastrointestinal tract in rodents. It mediates a reduction in food intake and body weight gain in rats upon treatment with oleoyl ethanolamide (OEA), an endogenous, potent agonist for PPARα. These data suggest that PSN632408 may be useful as a therapeutic agent for the treatment of obesity.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GPR119

Research Areas >> Metabolic Disease

[References]

[1]. Overton HA, et al. Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab. 2006 Mar;3(3):167-75.

[Related Small Molecules]

AR 231453 | MBX-2982 | JNJ-38431055 | GSK1292263 | APD 668 | Firuglipel

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
513.8±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₈H₂₄N₄O₄

[ Molecular Weight ]:
360.408

[ Flash Point ]:
264.5±32.9 °C

[ Exact Mass ]:
360.179749

[ PSA ]:
90.58000

[ LogP ]:
2.19

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.564

[ Storage condition ]:
2-8℃