APD668

APD668

中文名称APD668
中文同义词异丙基 4-(1-(2-氟-4-(甲基磺酰基)苯基)-1H-吡唑并[3,4-D]嘧啶-4-基氧基)哌啶-1-羧酸;4-(1-(2-氟-4-(甲磺酰基)苯基)-1H-吡唑并[3,4-D]嘧啶-4-氧基)哌啶-1-羧酸异丙酯;化合物APD 668;4-((1-(2-氟-4-(甲基磺酰基)苯基)-1H-吡唑并[3,4-D]嘧啶-4-基)氧基)哌啶-1-甲酸异丙酯
英文名称APD668
英文同义词APD668;APD668 ISOPROPYL 4-(1-(2-FLUORO-4-(METHYLSULFONYL)PHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLOXY)PIPERIDINE-1-CARBOXYLATE;isopropyl 4-((1-(2-fluoro-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)oxy)piperidine-1-carboxylate APD668;APD 668, >=98%;4-[[1-(2-Fluoro-4-methylsulfonylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]piperidine-1-carboxylic acid isopropyl ester;1-Piperidinecarboxylic acid,4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-, 1-methylethyl ester;APD 668; APD-668;CS-1179
CAS号832714-46-2
分子式C21H24FN5O5S
分子量477.51
EINECS号
相关类别小分子抑制剂;小分子抑制剂,天然产物;Inhibitors
Mol文件832714-46-2.mol
结构式APD668 结构式

APD668 性质

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
溶解度不溶于水; DMSO 中≥17.4 mg/mL;温和加热和超声波下,乙醇中≥2.61 mg/mL
形态固体
酸度系数(pKa)2.13±0.30(Predicted)
颜色白色至米白色

APD668 用途与合成方法

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。
TargetValue
human GPR119
()
2.7 nM(EC50)
rat GPR119
()
33 nM(EC50)

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.

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/08/19HY-15565APD6681 mg623元
2024/08/19HY-15565APD668
APD668
832714-46-25 mg1300元

APD668 上下游产品信息

"APD668"相关产品信息
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