2. Metabolic Enzyme/Protease
  3. Glucokinase
  4. AMG-1694

AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals.

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AMG-1694 Chemical Structure

AMG-1694 Chemical Structure

CAS No. : 1361217-07-3

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Based on 1 publication(s) in Google Scholar

AMG-1694 Related Antibodies

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Description

AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals[1].

IC50 & Target

IC50: 7 nM (GK-GKRP)[1]
Cellular Effect
Cell Line Type Value Description References
Hepatocyte EC50
0.082 μM
Compound: 25, AMG-1694
Inhibition of GKRP-GK interaction in rat primary hepatocytes assessed as translocation of GK from nucleus to cytoplasm preincubated for 20 mins followed by glucose addition measured after 40 mins by fluorescence assay
Inhibition of GKRP-GK interaction in rat primary hepatocytes assessed as translocation of GK from nucleus to cytoplasm preincubated for 20 mins followed by glucose addition measured after 40 mins by fluorescence assay
[PMID: 24405172]
Hepatocyte EC50
1.79 μM
Compound: 1, AMG-1694
Induction of GK translocation from nucleus to cytoplasm of mouse hepatocytes preincubated for 20 mins followed by glucose challenge measured after 40 mins by Hoechst 33342 staining-based assay
Induction of GK translocation from nucleus to cytoplasm of mouse hepatocytes preincubated for 20 mins followed by glucose challenge measured after 40 mins by Hoechst 33342 staining-based assay
[PMID: 24405213]
In Vitro

AMG-1694 is highly effective in restoring the enzymatic activity of GK with an EC50 of 0.020 μM in the presence of GKRP[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AMG-1694 Related Antibodies
Molecular Weight

533.63

Formula

C23H30F3N3O4S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

C[C@@](O)(C1=CC=C(N2[C@@H](CN3[C@@H](C)COCC3)CN(S(=O)(C4=CC=CS4)=O)CC2)C=C1)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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AMG-1694 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMG-16941361217-07-3AMG1694AMG 1694GlucokinaseHexokinase IVHexokinase DInhibitorinhibitorinhibit

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