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Medchemexpress LLC Amg-1694 | 1361217-07-3 | 533.63 | 25 MG
Supplier: Medchemexpress LLC 25MGHY12614
AMG-1694 is a potent glucokinase-glucokinase regulatory protein (GK-GKRP) disruptor. It promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, thereby indirectly increasing GK enzymatic activity. It effectively reverses the inhibitory effect of GKRP on GK activity and encourages GK translocation. In various rodent models of diabetes, AMG-1694 normalizes blood glucose levels, with its effect restricted to diabetic animals and not observed in normoglycemic ones.
- IC50 & target: 7 nM (GK-GKRP)
- Hepatocyte EC50: 0.082 μM (inhibition of GKRP-GK interaction in rat primary hepatocytes)
- Hepatocyte EC50: 1.79 μM (induction of GK translocation from nucleus to cytoplasm of mouse hepatocytes)
- In vitro: Effectively restores the enzymatic activity of GK with an EC50 of 0.020 μM in the presence of GKRP
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