918902-32-6
Chemical Structure
GPi688
- CAS No.: 918902-32-6
- Formula:C19H18ClN3O4S
- Molecular Weight:419.88
IUPAC Name: 2-chloro-N-(1-((R)-2,3-dihydroxypropyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide
InChIKey: UICNBXVDHCBKCE-PUODRLBUSA-N
SMILES: O=C(C1=CC(C=C(Cl)S2)=C2N1)NC3C(N(C[C@@H](O)CO)C4=C(C=CC=C4)C3)=O
Biological Activity: 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].
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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. GPi688 can inhibit glucagons-mediated glucose output in rat primary hepatocytes. GPi688 can be used for researching glucagon-mediated hyperglycaemia. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
