CP 316819 is a potent glycogen phosphorylase (GPase) inhibitor (antagonist) with hypoglycemic effects (IC50s for human skeletal muscle glycogen phosphorylase (huSMGPa) and liver glycogen phosphorylase (huLGPa) are respectively 17 nM and 34 nM). CP 316819 causes glycogen accumulation under normoglycemic conditions but allows glycogen utilization at lower glucose concentrations. CP-316819 prevents nerve cell death and maintains brain currents.

Physicochemical Properties

Molecular Formula	C21H22CLN3O4
Molecular Weight	415.87
Exact Mass	415.129
CAS #	186392-43-8
PubChem CID	10273347
Appearance	White to off-white solid powder
Density	1.4±0.1 g/cm3
Index of Refraction	1.649
LogP	4.52
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	7
Heavy Atom Count	29
Complexity	572
Defined Atom Stereocenter Count	2
SMILES	ClC1=CC=C2C(C=C(C(NC(CC3C=CC=CC=3)C(O)C(NCOC)=O)=O)N2)=C1
HS Tariff Code	2934.99.9001
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)

Biological Activity

References

[1]. Baker DJ, Timmons JA, Greenhaff PL. Glycogen phosphorylase inhibition in type 2 diabetes therapy: a systematic evaluation of metabolic and functional effects in rat skeletal muscle. Diabetes. 2005 Aug;54(8):2453-9. [2]. Suh SW, Bergher JP, Anderson CM, Treadway JL, Fosgerau K, Swanson RA. 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.

Solubility Data

Solubility (In Vitro)

DMSO: 125 mg/mL (300.57 mM)

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.