| Identification | Back Directory | [Name]
PSN632408 | [CAS]
857652-30-3 | [Synonyms]
PSN632408
PSN 632408; PSN-632408; PSN 632408; PSN-632408
tert-butyl 4-((3-(pyridin-4-yl)-1,2,4-oxadiazol-5-yl)methoxy)piperidine-1-carboxylate
1-Piperidinecarboxylic acid, 4-[[3-(4-pyridinyl)-1,2,4-oxadiazol-5-yl]methoxy]-, 1,1-dimethylethyl ester | [Molecular Formula]
C18H24N4O4 | [MDL Number]
MFCD09297322 | [MOL File]
857652-30-3.mol | [Molecular Weight]
360.41 |
| Chemical Properties | Back Directory | [Boiling point ]
513.8±60.0 °C(Predicted) | [density ]
1.25±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
crystalline solid | [pka]
0.79±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders[1][2]. | [Biological Activity]
psn632408 is a novel, selective and small-molecule agonist of human and mouse gpr119 with ec50 values of 5.6±0.99 μm and 7.9±0.7 μm, respectively [1].psn632408 has been reported to activate human and mouse gpr119 in a yeast fluorimetric assay with ec50 of 5.6±0.99 μm and 7.9±0.7 μm, respectively. in hek-osgpr116 cells, camp level was dose-dependently increased by psn632408 with an ec50 of 1.9±0.14 μm.. in vivo, psn632408 induced food intake reduction by using a rat feeding model and acute hypophagic effects in dose-dependence [1]. | [in vivo]
PSN632408 (100 mg/kg; p.o.; daily for 14 days) suppresses food intake in rats and reduce body weight gain and white adipose tissue deposition upon subchronic oral administration to high-fat-fed rats[1]. | Animal Model: | Diet-induced obese (DIO) rats[1] | | Dosage: | 100 mg/kg | | Administration: | P.o.; daily for 14 days | | Result: | The mean daily food intake was decreased by 10% during the first week of dosing and 15% during the second week. Body weight gain was significantly attenuated from day 6 onward with some evidence of weight loss.
|
| [References]
[1] overton ha1, babbs aj, doel sm, fyfe mc, gardner ls, griffin g, jackson hc, procter mj, rasamison cm, tang-christensen m, widdowson ps, williams gm, reynet c.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 |
|
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|