Biological Activity
Selective glycogen phosphorylase inhibitor [IC50 values are 0.017 and 0.034 μM against human skeletal muscle glycogen phosphorylase a (huSMGPa) and liver glycogen phosphorylase a (huLGPa) respectively]. Antihyperglycemic agent.
Compound Libraries
CP 316819 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 415.87 |
| Formula | C21H22ClN3O4 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 186392-43-8 |
| PubChem ID | 10273347 |
| InChI Key | WEQLRDLTRCEUHG-PKOBYXMFSA-N |
| Smiles | O=C(N[C@@H](CC3=CC=CC=C3)[C@H](C(N(OC)C)=O)O)C2=CC1=CC(Cl)=CC=C1N2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.59 | 100 | |
| ethanol | 41.59 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 415.87. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.4 mL | 12.02 mL | 24.05 mL |
| 5 mM | 0.48 mL | 2.4 mL | 4.81 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.4 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Baker et al (2005) Glycogen phosphorylase inhibition in type 2 diabetes therapy: a systematic evaluation of metabolic and functional effects in rat skeletal muscle. Diabetes 54 2453 PMID: 16046314
Freeman et al (2006) Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation site of the enzyme. Br.J.Pharmacol. 149 775 PMID: 17016495
Suh et al (2007) Astrocyte glycogen sustains neuronal activity during hypoglycemia: studies with the glycogen phosphorylase inhibitor CP-316,819 ([R-R*,S*]-5-chloro-N-[2-hydroxy-3-(methoxymethylamino)-3-oxo-1-(phenylmethyl)propyl]-1H-indole-2-ca J.Pharmacol.Exp.Ther. 321 45 PMID: 17251391
Keywords: CP 316819, supplier, glycogen, phosphorylase, inhibitors, inhibits, antihyperglycemic, antihyperglycaemic, transferases, carbohydrate, metabolism, CP316819, Phosphorylases, Phosphorylases, Tocris Bioscience
