| Bioactivity | 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]. | |||||||||
| Invitro | PSN632408 produces concentration-dependent increases in cAMP level with mean EC50 value of 1.9 uM[1].PSN632408 stimulates β cell replication in cultured mouse islets[2]. | |||||||||
| 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: | |||||||||
| Name | PSN632408 | |||||||||
| CAS | 857652-30-3 | |||||||||
| Formula | C18H24N4O4 | |||||||||
| Molar Mass | 360.41 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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;3(3):167-175. [2]. Gao J, et al. Stimulating beta cell replication and improving islet graft function by GPR119 agonists. Transpl Int. 2011;24(11):1124-1134. |