APD668
- CAS号:832714-46-2
- 英文名:APD668
- 中文名:APD668
- CBNumber:CB62667083
- 分子式:C21H24FN5O5S
- 分子量:477.51
- MOL File:832714-46-2.mol
- 沸点 :611.6±55.0 °C(Predicted)
- 密度 :1.47±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :insoluble in H2O; ≥17.4 mg/mL in DMSO; ≥2.61 mg/mL in EtOH with gentle warming and ultrasonic
- 形态 :solid
- 酸度系数(pKa) :2.13±0.30(Predicted)
- 颜色 :White to off-white
APD668性质、用途与生产工艺
- 生物活性 APD668是有效的GPR119激动剂,对人源GPR119和大鼠GPR119的EC50值分别为2.7 nM和33 nM。
-
靶点
Target Value human GPR119
()2.7 nM(EC50) rat GPR119
()33 nM(EC50) -
体外研究
APD668 increases adenylate cyclase activation in HEK293 cells transfected with human GPR119 in a concentration-dependent manner with an EC 50 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 (t max ≤2 h) in mice, rats, and monkeys, but slower in dogs (t max =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.
- 更新日期:2024/11/11
- 产品编号:XW83271446201
- 产品名称:试剂APD668 APD668
- CAS编号:
- 包装:50mg
- 价格:459元
- 更新日期:2024/11/08
- 产品编号:HY-15565
- 产品名称:APD668
- CAS编号:
- 包装:1 mg
- 价格:623元
- 公司名称:上海波以尔化工有限公司
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