918902-32-6

918902-32-6 structure

Name: GPi 688
Chemical Name: 6H-Thieno[2,3-b]pyrrole-5-carboxamide, 2-chloro-N-[1-[(2R)-2,3-dihydroxypropyl]-1,2,3,4-tetrahydro-2-oxo-3-quinolinyl]
CAS Number: 918902-32-6
Molecular Formula: C₁₉H₁₈ClN₃O₄S
Molecular Weight: 419.88
Catalog: Research Areas Metabolic Disease
Create Date: 2016-07-23 20:54:22
Modify Date: 2024-01-11 17:38:33
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].

Name	6H-Thieno[2,3-b]pyrrole-5-carboxamide, 2-chloro-N-[1-[(2R)-2,3-dihydroxypropyl]-1,2,3,4-tetrahydro-2-oxo-3-quinolinyl]
Synonyms	GPi 688

Description	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].
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Metabolic Disease
Target	IC50: 19 nM (human liver GPa), 61 nM (rat liver GPa), 12 nM (human skeletal muscle GPa)[1]
References	[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.