S88718 |
APD668 |
| 源叶(MedMol) | 95% |
- 产品描述： APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes
- 靶点： CYP2C9:0.1 μM (Ki);hGPR119:2.7 nM (IC50);rGPR119:33 nM (IC50);hERG channel:3 μM (IC50)
- 体外研究： APD668 increases adenylate cyclase activation in HEK293 cells transfected with human GPR119 in a concentration-dependent manner with an EC50 of 23 nM. APD668 is highly bound to plasma proteins of male and female cynomolgus monkeys and humans (⩾99%), but is less extensively bound to male (93.0%) and female (96.6%) rats
- 体内研究： APD668 (10-30 mg/kg; p.o. once daily for 8 weeks) significantly reduces blood glucose and glycated hemoglobin (HbA1c) levels, with no desensitization of the acute drug response. APD668 (1-10 mg/kg; a single p.o.) markedly reduces blood glucose levels during oral glucose tolerance test in a dose-dependent manner in mice. APD668 (0.08 mg/kg/min; i.v.) shows no effect during euglycemic condition, but significantly stimulates insulin release when blood glucose levels are raised to approximately 300 mg/dl in a hyperglycemic clamp model in the Sprague-Dawley rat. APD668 (p.o.) exhibits rapid to moderate absorption (tmax≤2 h) in mice, rats, and monkeys, but slower in dogs (tmax=6 h), and moderate to good absolute oral bioavailability (44-79%) in mice, rats, and monkeys, but lower in dogs (22%). Animal Model: Male Zucker Diabetic Fatty (ZDF) rats (6 weeks old, 200-250 g) Dosage: 10, 30 mg/kg Administration: P.o. once daily for 8 weeks Result: Decreased the blood glucose and HbA1c levels at 30 mg/kg/day.Did not develop diabetes, whereas the vehicle treated rats did.
- 参考文献：
1. Semple G, 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 May 15;21(10):3134-41. 2. Bahirat UA, et, al. APD668, a G protein-coupled receptor 119 agonist improves fat tolerance and attenuates fatty liver in high-trans fat diet induced steatohepatitis model in C57BL/6 mice. Eur J Pharmacol. 2017 Apr 15;801:35-45.
- 溶解性： Soluble in DMSO
- 保存条件： -20°C
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.094 ml 10.471 ml 20.942 ml 5 mM 0.419 ml 2.094 ml 4.188 ml 10 mM 0.209 ml 1.047 ml 2.094 ml 50 mM 0.042 ml 0.209 ml 0.419 ml
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