生物活性 靶点 体外研究 体内研究 APD668 试剂级价格
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APD668

APD668,832714-46-2,结构式
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
APD668化学性质
  • 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 :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
    TargetValue
    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.
APD668上下游产品信息
上游原料
下游产品
APD668 试剂级价格
  • 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
APD668生产厂家
  • 公司名称:MedChemexpress LLC
  • 联系电话:021-58955995
  • 电子邮件:sales@medchemexpress.cn
  • 国家:美国
  • 产品数:4861
  • 优势度:58
  • 公司名称:AdooQ BioScience, LLC
  • 联系电话:+1 (866) 930-6790
  • 电子邮件:info@adooq.com
  • 国家:美国
  • 产品数:2782
  • 优势度:58