产品
编 号：F120952
分子式：C27H20F2N2O7S2
分子量：586.58
分子式：C27H20F2N2O7S2
分子量：586.58
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CAS No: 1328987-85-4
产品详情
生物活性：
Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.
体内研究：
Glucokinase activator 1 (3 to 300 mg/kg, oral, 180 minutes) shows a dose dependent improvement in glucose excursion in oGTT in a DIO mouse model of T2D. The predominant liver-directed tissue distribution of Glucokinase activator 1 ensures a good safety window with respect to hypoglycemia over a 10-fold dose range.Animal Model:Male C57BL/6J mice (age 8-10 weeks; 25±5 g)
Dosage:1 or 3 mg/kg (i.v.), 30 mg/kg (oral)
Administration:I.v. or oral
Result:Showed an excellent PK profile and exhibited 35- and 68- fold higher liver concentrations at 1 and 3 h time point, respectively, compared with plasma.
Animal Model:Male C57BL/6J mice of 10-12 weeks
Dosage:3 to 300 mg/kg
Administration:Oral (15, 30, 60, 120 and 180 minutes)
Result:Demonstrated 21% and 34% significant AUC glucose reduction at oral dose of 30 and 100 mg/kg, respectively.
Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.
体内研究：
Glucokinase activator 1 (3 to 300 mg/kg, oral, 180 minutes) shows a dose dependent improvement in glucose excursion in oGTT in a DIO mouse model of T2D. The predominant liver-directed tissue distribution of Glucokinase activator 1 ensures a good safety window with respect to hypoglycemia over a 10-fold dose range.Animal Model:Male C57BL/6J mice (age 8-10 weeks; 25±5 g)
Dosage:1 or 3 mg/kg (i.v.), 30 mg/kg (oral)
Administration:I.v. or oral
Result:Showed an excellent PK profile and exhibited 35- and 68- fold higher liver concentrations at 1 and 3 h time point, respectively, compared with plasma.
Animal Model:Male C57BL/6J mice of 10-12 weeks
Dosage:3 to 300 mg/kg
Administration:Oral (15, 30, 60, 120 and 180 minutes)
Result:Demonstrated 21% and 34% significant AUC glucose reduction at oral dose of 30 and 100 mg/kg, respectively.
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