Glucokinase activator 1

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CAS NO:

1328987-85-4

Glucokinase activator 1 是针对肝脏的葡萄糖激酶活化剂，EC₅₀为34 nM。

生物活性

Glucokinase activator1 is a liver-directedglucokinaseactivator with anEC₅₀of 34 nM.

IC₅₀& Target

EC50: 34 nM (Glucokinase)^[1]

体内研究
(In Vivo)

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^[1].

Animal Model:	Male C57BL/6J mice (age 8-10 weeks; 25±5 g)^[1]
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^[1].

Animal Model:	Male C57BL/6J mice of 10-12 weeks^[1]
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^[1].

分子量

586.58

Formula

C₂₇H₂₀F₂N₂O₇S₂

CAS 号

1328987-85-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.