GPi688

GPi688 is a potent and orally active glycogen phosphorylase (GPa) inhibitor with IC50s of 19 nM, 61 nM and 12 nM for human liver GPa, rat liver GPa and human skeletal muscle GPa, respectively[1]. GPi688 can inhibit glucagons-mediated glucose output in rat primary hepatocytes. GPi688 can be used for researching glucagon-mediated hyperglycaemia[2].

Product Specifications

CAS Number

[918902-32-6]

UNSPSC

12352005

Target

Phosphorylase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/gpi688.html

Solubility

10 mM in DMSO

Smiles

O=C(C1=CC(C=C(Cl)S2)=C2N1)NC3C(N(C[C@@H](O)CO)C4=C(C=CC=C4)C3)=O

Molecular Formula

C19H18ClN3O4S

Molecular Weight

419.88

References & Citations

[1]Freeman S, et al. Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation state of the enzyme. Br J Pharmacol. 2006;149 (6) :775-785.|[2]Poucher SM, et al. An assessment of the in vivo efficacy of the glycogen phosphorylase inhibitor GPi688 in rat models of hyperglycaemia. Br J Pharmacol. 2007;152 (8) :1239-1247.