| 产品描述: | 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 |
| 靶点: |
GPR119 |
| 体外研究: |
PSN632408 produces concentration-dependent increases in cAMP level with mean EC50 value of 1.9 uM. PSN632408 stimulates β cell replication in cultured mouse islets |
| 体内研究: |
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. Animal Model: Diet-induced obese (DIO) rats 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 |
| 参考文献: |
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. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.775 ml |
13.873 ml |
27.746 ml |
| 5 mM |
0.555 ml |
2.775 ml |
5.549 ml |
| 10 mM |
0.277 ml |
1.387 ml |
2.775 ml |
| 50 mM |
0.055 ml |
0.277 ml |
0.555 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |