APD668
ISOPROPYL 4-(1-(2-FLUORO-4-(METHYLSULFONYL)PHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLOXY)PIPERIDINE-1-CARBOXYLATE
CAS: 832714-46-2
Molecular Formula: C21H24FN5O5S
APD668 - Names and Identifiers
APD668 - Physico-chemical Properties
| Molecular Formula | C21H24FN5O5S |
| Molar Mass | 477.51 |
| Density | 1.47±0.1 g/cm3(Predicted) |
| Boling Point | 611.6±55.0 °C(Predicted) |
| Solubility | DMSO : 33.33 mg/mL (69.80 mM; Need ultrasonic);H2O : < 0.1 mg/mL (insoluble) |
| pKa | 2.13±0.30(Predicted) |
| Storage Condition | -20°C |
| In vitro study | 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. |
| In vivo study | 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 - Preparation solution concentration reference
| 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 |
| 5 mM | 0.042 ml | 0.209 ml | 0.419 ml |
Last Update：2024-01-02 23:10:35
APD668 - Reference Information
| biological activity | APD668 is an effective GPR119 agonist, and the EC50 values for human GPR119 and rat GPR119 are 2.7 nM and 33 nM respectively. |
| target | TargetValue human GPR119 () 2.7 nM(EC50) rat GPR119 () 33 nM(EC50) |
| Target | Value |
| human GPR119 () | 2.7 nM(EC50) |
| rat GPR119 () | 33 nM(EC50) |
| in vitro study | 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 high 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. |
| in vivo study | 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 slow 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, 200-250g) 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 ats did. |
| 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. |
Last Update：2024-04-09 21:01:54
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Product Name: ISOPROPYL 4-(1-(2-FLUORO-4-(METHYLSULFONYL)PHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLOXY)PIPERIDINE-1-CARBOXYLATE Visit Supplier Webpage Request for quotationCAS: 832714-46-2
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Product Name: ISOPROPYL 4-(1-(2-FLUORO-4-(METHYLSULFONYL)PHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLOXY)PIPERIDINE-1-CARBOXYLATE Visit Supplier Webpage Request for quotationCAS: 832714-46-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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