产品
编 号：F472480
分子式：C21H24FN5O5S
分子量：477.51
分子式：C21H24FN5O5S
分子量：477.51
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 832714-46-2
产品详情
生物活性：
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.
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.
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.
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.
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.
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.
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