1328987-85-4
1328987-85-4 structure
- Name: Glucokinase activator 1
- Chemical Name: Glucokinase activator 1
- CAS Number: 1328987-85-4
- Molecular Formula: C27H20F2N2O7S2
- Molecular Weight: 586.58
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Glucokinase
- Create Date: 2019-03-30 23:37:34
- Modify Date: 2025-09-01 15:50:33
-
Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.
| Name | Glucokinase activator 1 |
|---|
| 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 |
| Molecular Formula | C27H20F2N2O7S2 |
|---|---|
| Molecular Weight | 586.58 |