| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Glycogen phosphorylase (GPase). Specifically, it targets the skeletal muscle (huSMGPa) and liver (huLGPa) isozymes.
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| ln Vitro |
CP-316819 is a potent inhibitor of glycogen phosphorylase A, with an IC50 of 40 nM for the human liver enzyme. At a concentration of 10 µM, it increases intracellular glycogen content in astrocytes. It inhibits huSMGPa with an IC50 of 17 nM and huLGPa with an IC50 of 34 nM.
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| ln Vivo |
In vivo, CP-316819 has antihyperglycemic effects. It leads to glycogen accumulation under normoglycemic conditions but allows glycogen utilization when glucose concentrations are low. It prevents neuronal cell death and maintains brain currents, suggesting a neuroprotective role during hypoglycemia.
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| Enzyme Assay |
The inhibitory activity of CP-316819 on glycogen phosphorylase is measured using an in vitro enzyme assay. The enzyme (e.g., huSMGPa or huLGPa) is incubated with its substrate (glycogen) and inorganic phosphate in the presence of varying concentrations of the inhibitor. The release of glucose-1-phosphate is measured, and the IC50 is determined from a dose-response curve.
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| Cell Assay |
The effect of CP-316819 on glycogen metabolism is studied in cells like astrocytes. Cells are treated with the compound, and the intracellular glycogen content is measured using a glycogen assay kit. The effect on cell viability and function under hypoglycemic conditions can also be assessed to evaluate its neuroprotective potential.
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| Animal Protocol |
The in vivo efficacy of CP-316819 is evaluated in animal models of diabetes or hypoglycemia. The compound is administered (route and dose vary), and blood glucose levels are monitored. In models of hypoglycemic neuronal injury, parameters like neuronal survival and brain electrical activity are assessed.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for CP-316819 are not widely published. As a small molecule (MW 415.87), it would be expected to be orally bioavailable. Its solubility and stability would be characterized during its development as a potential therapeutic agent. Standard storage at -20°C is recommended.
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| Toxicity/Toxicokinetics |
Toxicological data for CP-316819 are not available in general references. As a research compound, it is not intended for human use. Its safety profile would be established through preclinical toxicology studies if it were to be developed further.
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| References |
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| Additional Infomation |
CP-316819 is a research compound developed by Pfizer as a potential treatment for glycemic control. Its mechanism of inhibiting glycogen phosphorylase represents a strategy for reducing hepatic glucose output and managing hyperglycemia. It has also been studied for its neuroprotective effects, making it a tool to investigate the role of glycogen metabolism in the brain.
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| Molecular Formula |
C21H22CLN3O4
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|---|---|
| Molecular Weight |
415.87
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| Exact Mass |
415.129
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| CAS # |
186392-43-8
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| PubChem CID |
10273347
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.649
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| LogP |
4.52
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
572
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| Defined Atom Stereocenter Count |
2
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| SMILES |
ClC1=CC=C2C(C=C(C(NC(CC3C=CC=CC=3)C(O)C(NCOC)=O)=O)N2)=C1
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| InChi Key |
WEQLRDLTRCEUHG-PKOBYXMFSA-N
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| InChi Code |
InChI=1S/C21H22ClN3O4/c1-25(29-2)21(28)19(26)17(10-13-6-4-3-5-7-13)24-20(27)18-12-14-11-15(22)8-9-16(14)23-18/h3-9,11-12,17,19,23,26H,10H2,1-2H3,(H,24,27)/t17-,19+/m0/s1
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| Chemical Name |
5-chloro-N-[(2S,3R)-3-hydroxy-4-[methoxy(methyl)amino]-4-oxo-1-phenylbutan-2-yl]-1H-indole-2-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (300.57 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4046 mL | 12.0230 mL | 24.0460 mL | |
| 5 mM | 0.4809 mL | 2.4046 mL | 4.8092 mL | |
| 10 mM | 0.2405 mL | 1.2023 mL | 2.4046 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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