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cp-316819  (Pfizer Inc)

 
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    Structured Review

    Pfizer Inc cp-316819
    Structures of GPi‐s. (A) KB228, 3 μM final concentration (Ki = 937 nM). (B) BEVA335, 1.5 μM final concentration (Ki = 411 nM). (C) <t>CP‐316819,</t> 0.5 μM final concentration (Ki = 209 nM). (D) Kinetics of inhibition of glycogen phosphorylase b by CP316819 was analysed at a constant concentration of glycogen (1 m·V−1%) and various concentrations of glucose‐1‐phosphate (4–40 mM). The slopes of double reciprocal plots against the effective inhibitor concentrations were replotted to give the secondary plots, which were analysed and showed the Ki for the inhibitor.
    Cp 316819, supplied by Pfizer Inc, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/cp-316819/cp+316+311/pmc05758390-702-1-2
    Average 90 stars, based on 1 article reviews
    cp-316819 - by Bioz Stars, 2026-09
    90/100 stars

    Images

    1) Product Images from "Glycogen phosphorylase inhibition improves beta cell function"

    Article Title: Glycogen phosphorylase inhibition improves beta cell function

    Journal: British Journal of Pharmacology

    doi: 10.1111/bph.13819

    Structures of GPi‐s. (A) KB228, 3 μM final concentration (Ki = 937 nM). (B) BEVA335, 1.5 μM final concentration (Ki = 411 nM). (C) CP‐316819, 0.5 μM final concentration (Ki = 209 nM). (D) Kinetics of inhibition of glycogen phosphorylase b by CP316819 was analysed at a constant concentration of glycogen (1 m·V−1%) and various concentrations of glucose‐1‐phosphate (4–40 mM). The slopes of double reciprocal plots against the effective inhibitor concentrations were replotted to give the secondary plots, which were analysed and showed the Ki for the inhibitor.
    Figure Legend Snippet: Structures of GPi‐s. (A) KB228, 3 μM final concentration (Ki = 937 nM). (B) BEVA335, 1.5 μM final concentration (Ki = 411 nM). (C) CP‐316819, 0.5 μM final concentration (Ki = 209 nM). (D) Kinetics of inhibition of glycogen phosphorylase b by CP316819 was analysed at a constant concentration of glycogen (1 m·V−1%) and various concentrations of glucose‐1‐phosphate (4–40 mM). The slopes of double reciprocal plots against the effective inhibitor concentrations were replotted to give the secondary plots, which were analysed and showed the Ki for the inhibitor.

    Techniques Used: Concentration Assay, Inhibition

    Related Articles

    Concentration Assay:

    Article Title: Glycogen phosphorylase inhibition in type 2 diabetes therapy: a systematic evaluation of metabolic and functional effects in rat skeletal muscle.
    Article Snippet: In one group of animals (GPi, n 30), CP-316819 (Pfizer Global R&D; IC50 against glycogen phosphorylase, 100 nmol/l; IC50 on cell glycogenolysis, 1.5 mol/l; dissolved in DMSO) was added to the perfusion medium to give an unbound free drug concentration of 3 mol/l and DMSO concentration of 0.01%, whereas the control group (n 29) received vehicle only.

    Article Title: Glycogen phosphorylase inhibition improves beta cell function
    Article Snippet: Namely, CP‐316819 (Pfizer, a drug used in our current study), {"type":"entrez-protein","attrs":{"text":"AVE56588","term_id":"1344835984","term_text":"AVE56588"}} AVE56588 (Sanofi‐Aventis) and GSK1362885 (GlaxoSmithKline) completed phase I, while CP‐368296 (Ingliforib, Pfizer) and PSN‐357 (Prosidion, now Astellas Pharma) advanced to phase II (for review, see Henke, 2012 ).

    Article Title: A glycogen phosphorylase inhibitor selectively enhances local rates of glucose utilization in brain during sensory stimulation of conscious rats: implications for glycogen turnover
    Article Snippet: We thank Pfizer Global Research and Development, Groton, CT, USA, for generously providing CP-316819 and W. Ross Tracey, PhD, Department of Cardiovascular, Metabolic and Endocrine Diseases, Pfizer, for his sponsorship of our request.

    Inhibition:

    Article Title: Glycogen phosphorylase inhibition in type 2 diabetes therapy: a systematic evaluation of metabolic and functional effects in rat skeletal muscle.
    Article Snippet: In one group of animals (GPi, n 30), CP-316819 (Pfizer Global R&D; IC50 against glycogen phosphorylase, 100 nmol/l; IC50 on cell glycogenolysis, 1.5 mol/l; dissolved in DMSO) was added to the perfusion medium to give an unbound free drug concentration of 3 mol/l and DMSO concentration of 0.01%, whereas the control group (n 29) received vehicle only.

    Article Title: Glycogen phosphorylase inhibition improves beta cell function
    Article Snippet: Namely, CP‐316819 (Pfizer, a drug used in our current study), {"type":"entrez-protein","attrs":{"text":"AVE56588","term_id":"1344835984","term_text":"AVE56588"}} AVE56588 (Sanofi‐Aventis) and GSK1362885 (GlaxoSmithKline) completed phase I, while CP‐368296 (Ingliforib, Pfizer) and PSN‐357 (Prosidion, now Astellas Pharma) advanced to phase II (for review, see Henke, 2012 ).

    Article Title: A glycogen phosphorylase inhibitor selectively enhances local rates of glucose utilization in brain during sensory stimulation of conscious rats: implications for glycogen turnover
    Article Snippet: We thank Pfizer Global Research and Development, Groton, CT, USA, for generously providing CP-316819 and W. Ross Tracey, PhD, Department of Cardiovascular, Metabolic and Endocrine Diseases, Pfizer, for his sponsorship of our request.

    Control:

    Article Title: Glycogen phosphorylase inhibition in type 2 diabetes therapy: a systematic evaluation of metabolic and functional effects in rat skeletal muscle.
    Article Snippet: In one group of animals (GPi, n 30), CP-316819 (Pfizer Global R&D; IC50 against glycogen phosphorylase, 100 nmol/l; IC50 on cell glycogenolysis, 1.5 mol/l; dissolved in DMSO) was added to the perfusion medium to give an unbound free drug concentration of 3 mol/l and DMSO concentration of 0.01%, whereas the control group (n 29) received vehicle only.

    Article Title: Glycogen phosphorylase inhibition improves beta cell function
    Article Snippet: Namely, CP‐316819 (Pfizer, a drug used in our current study), {"type":"entrez-protein","attrs":{"text":"AVE56588","term_id":"1344835984","term_text":"AVE56588"}} AVE56588 (Sanofi‐Aventis) and GSK1362885 (GlaxoSmithKline) completed phase I, while CP‐368296 (Ingliforib, Pfizer) and PSN‐357 (Prosidion, now Astellas Pharma) advanced to phase II (for review, see Henke, 2012 ).

    Article Title: A glycogen phosphorylase inhibitor selectively enhances local rates of glucose utilization in brain during sensory stimulation of conscious rats: implications for glycogen turnover
    Article Snippet: We thank Pfizer Global Research and Development, Groton, CT, USA, for generously providing CP-316819 and W. Ross Tracey, PhD, Department of Cardiovascular, Metabolic and Endocrine Diseases, Pfizer, for his sponsorship of our request.



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    Structures of GPi‐s. (A) KB228, 3 μM final concentration (Ki = 937 nM). (B) BEVA335, 1.5 μM final concentration (Ki = 411 nM). (C) <t>CP‐316819,</t> 0.5 μM final concentration (Ki = 209 nM). (D) Kinetics of inhibition of glycogen phosphorylase b by CP316819 was analysed at a constant concentration of glycogen (1 m·V−1%) and various concentrations of glucose‐1‐phosphate (4–40 mM). The slopes of double reciprocal plots against the effective inhibitor concentrations were replotted to give the secondary plots, which were analysed and showed the Ki for the inhibitor.
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    https://www.bioz.com/product/cp-316819/cp+316+311/pmc05758390-702-1-2
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    Image Search Results


    Structures of GPi‐s. (A) KB228, 3 μM final concentration (Ki = 937 nM). (B) BEVA335, 1.5 μM final concentration (Ki = 411 nM). (C) CP‐316819, 0.5 μM final concentration (Ki = 209 nM). (D) Kinetics of inhibition of glycogen phosphorylase b by CP316819 was analysed at a constant concentration of glycogen (1 m·V−1%) and various concentrations of glucose‐1‐phosphate (4–40 mM). The slopes of double reciprocal plots against the effective inhibitor concentrations were replotted to give the secondary plots, which were analysed and showed the Ki for the inhibitor.

    Journal: British Journal of Pharmacology

    Article Title: Glycogen phosphorylase inhibition improves beta cell function

    doi: 10.1111/bph.13819

    Figure Lengend Snippet: Structures of GPi‐s. (A) KB228, 3 μM final concentration (Ki = 937 nM). (B) BEVA335, 1.5 μM final concentration (Ki = 411 nM). (C) CP‐316819, 0.5 μM final concentration (Ki = 209 nM). (D) Kinetics of inhibition of glycogen phosphorylase b by CP316819 was analysed at a constant concentration of glycogen (1 m·V−1%) and various concentrations of glucose‐1‐phosphate (4–40 mM). The slopes of double reciprocal plots against the effective inhibitor concentrations were replotted to give the secondary plots, which were analysed and showed the Ki for the inhibitor.

    Article Snippet: Namely, CP‐316819 (Pfizer, a drug used in our current study), {"type":"entrez-protein","attrs":{"text":"AVE56588","term_id":"1344835984","term_text":"AVE56588"}} AVE56588 (Sanofi‐Aventis) and GSK1362885 (GlaxoSmithKline) completed phase I, while CP‐368296 (Ingliforib, Pfizer) and PSN‐357 (Prosidion, now Astellas Pharma) advanced to phase II (for review, see Henke, 2012 ).

    Techniques: Concentration Assay, Inhibition