CP-91149 - CAS 186392-40-5
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Not Intended for Therapeutic Use. For research use only.
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Glycogen phosphorylase (GP)
CP-91149 is a selective glycogen phosphorylase (GP) inhibitor with IC50 of 0.13 μM in the presence of glucose, 5- to 10-fold less potent in the absence of glucose.
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1.Regulation of glycogen metabolism in cultured human muscles by the glycogen phosphorylase inhibitor CP-91149.
Lerín C1, Montell E, Nolasco T, García-Rocha M, Guinovart JJ, Gómez-Foix AM. Biochem J. 2004 Mar 15;378(Pt 3):1073-7.
Pharmacological inhibition of liver GP (glycogen phosphorylase), which is currently being studied as a treatment for Type II (non-insulin-dependent) diabetes, may affect muscle glycogen metabolism. In the present study, we analysed the effects of the GP inhibitor CP-91149 on non-engineered or GP-overexpressing cultured human muscle cells. We found that CP-91149 treatment decreased muscle GP activity by (1) converting the phosphorylated AMP-independent a form into the dephosphorylated AMP-dependent b form and (2) inhibiting GP a activity and AMP-mediated GP b activation. Dephosphorylation of GP was exerted, irrespective of incubation of the cells with glucose, whereas inhibition of its activity was synergic with glucose. As expected, CP-91149 impaired the glycogenolysis induced by glucose deprivation. CP-91149 also promoted the dephosphorylation and activation of GS (glycogen synthase) in non-engineered or GP-overexpressing cultured human muscle cells, but exclusively in glucose-deprived cells.
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CAS 186392-40-5 CP-91149

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