Glucokinase activator 1

Modify Date: 2024-01-05 17:36:47

Glucokinase activator 1 Structure
Glucokinase activator 1 structure
Common Name Glucokinase activator 1
CAS Number 1328987-85-4 Molecular Weight 586.58
Density N/A Boiling Point N/A
Molecular Formula C27H20F2N2O7S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Glucokinase activator 1


Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.

 Names

Name Glucokinase activator 1

 Glucokinase activator 1 Biological Activity

Description Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.
Related Catalog
Target

EC50: 34 nM (Glucokinase)[1]

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: Glucokinase activator 1 shows 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: Glucokinase activator 1 demonstrates 21% and 34% significant AUCglucose 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.

 Chemical & Physical Properties

Molecular Formula C27H20F2N2O7S2
Molecular Weight 586.58