1. Metabolic Enzyme/Protease
  2. Glucokinase
  3. Glucokinase activator 1

Glucokinase activator 1 

Cat. No.: HY-101788
Handling Instructions

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

For research use only. We do not sell to patients.

Glucokinase activator 1 Chemical Structure

Glucokinase activator 1 Chemical Structure

CAS No. : 1328987-85-4

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Description

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

IC50 & 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: 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].
Molecular Weight

586.58

Formula

C₂₇H₂₀F₂N₂O₇S₂

CAS No.

1328987-85-4

SMILES

O=S(C1=CC=C([[email protected]](C(NC2=NC=C(OC3=CC=C(C(O)=O)C=C3)S2)=O)OC4=CC=C(F)C=C4F)C=C1)(C5CC5)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage

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

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Glucokinase activator 1
Cat. No.:
HY-101788
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