- PSN 375963 hydrochloride
- MBX-2982
- AS 1269574
- PSN632408
| APD668Potent GPR119 agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.09%
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| Cas No. | 832714-46-2 | SDF | Download SDF |
| Formula | C21H24FN5O5S | M.Wt | 477.51 |
| Solubility | ≥17.4mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
APD688 is a selective and potent G protein-coupled receptor 119 (GPR119) agonist with an EC50 value of 2.7 nM for hGPR119 and 33 nM for rGPR119, and showed a moderate inhibition of the hERG channel (IC50 = 3 ?M), exhibiting an in vivo activity of glucose regulation in rodent models [1].
GPR199, which is predominantly expressed in human and rodent pancreas, is a membrane receptor that plays a role in the production of insulin as a response to high glucose concentration in male Wistar rats, and is a probable target for the treatment of diabetes [2]. GPR199 is also localized in the gastrointestinal track, providing a potential target for obesity therapy and other related metabolic disorders through reduced food intake [3].
In HEK293 cells transfected with human GPR119, application of APD688 displayed an increase in adenylatecyclase activation subsequently leading to enhanced release of insulin in a glucose-dependent manner [1].
Oral administration of APD688 in Zucker Diabetic Fatty (ZDF) rats for over 8 weeks resulted in the significant decrease in blood glucose and glycated hemoglobin (HbA1c) levels. In addition, the compound is mostly non-genotoxic, and shows no significant inhibition of CYP isoforms except for CYP2C9 (Ki = 0.1 ?M) in human hepatic microsomes [1].
References:[1]. Semple G, Ren A, Fioravanti B, et al. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg Med Chem Lett, 2011, 21(10):3134-41.[2]. Soga T, Ohishi T, Matsui T, et al. Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor. Biochem Biophys Res Commun, 2005, 326(4):744-51. [3]. Overton HA, Babbs AJ, Doel SM, 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):167-75.
