| Identification | Back Directory | [Name]
Glucokinase activator 1 | [CAS]
1328987-85-4 | [Synonyms]
Glucokise activator 1
Glucokinase activator 1
Benzoic acid, 4-[[2-[[(2R)-2-[4-(cyclopropylsulfonyl)phenyl]-2-(2,4-difluorophenoxy)acetyl]amino]-5-thiazolyl]oxy]- | [Molecular Formula]
C27H20F2N2O7S2 | [MDL Number]
MFCD31813602 | [MOL File]
1328987-85-4.mol | [Molecular Weight]
586.58 |
| Hazard Information | Back Directory | [Uses]
Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM. | [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]. |
| [References]
[1] Deshpande AM, et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur J Med Chem. 2017 Jun 16;133:268-286. DOI:10.1016/j.ejmech.2017.03.042 |
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