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CP-91149

Catalog No. T6455 CAS 186392-40-5

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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CP-91149, CAS 186392-40-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 76.00
25 mg	In stock	$ 155.00
50 mg	In stock	$ 247.00
100 mg	In stock	$ 358.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.81%

Purity: 99.75%

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Description	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.
Targets&IC50	GP:0.13 μM
In vitro	CP-91149 displays 200-fold higher inhibitory activity against human liver glycogen phosphorylase a (HLGPa) than caffeine (IC50 = 26 μM). CP-91149 (10-100 μM) inhibits glucagon-stimulated glycogenolysis in isolated rat hepatocytes in a dose-dependent manner, and in primary human hepatocytes with IC50 of ~2.1 μM. [1] CP-91149 also potently inhibits the activities of human muscle phosphorylase a and b with IC50 of 0.2 μM and ~0.3 μM, respectively. CP-91149 treatment at 2.5 μM induces inactivation of phosphorylase and sequential activation of glycogen synthase in hepatocytes, and increases glycogen synthesis by 7-fold at 5 mM glucose and by 2-fold at 20 mM glucose. CP-91149 can partially counteract the effects of phosphorylase overexpression. [2] CP-91149 also potently inhibits brain GP with IC50 of 0.5 μM in A549 cells. CP-91149 treatment at 10-30 μM causes significant glycogen accumulation in A549 and HSF55 cells. CP-91149 treatment increases G1-phase cells with a significant reduction of the S-phase population in HSF55 cells, correlated with increased expression of p21 and p27. [3] CP-91149 also promotes the dephosphorylation and activation of GS (glycogen synthase) in non-engineered or GP-overexpressing cultured human muscle cells, but exclusively in glucose-deprived cells. [4]
In vivo	Oral administration of CP-91149 to diabetic ob/ob mice at 25-50 mg/kg causes rapid (3 hours) glucose lowering by 100-120 mg/dl without producing hypoglycemia, resulting from inhibition of glycogenolysis in vivo. CP-91149 treatment does not lower glucose levels in normoglycemic, nondiabetic mice. [1] In the non-fasted Goto-Kakizaki (GK) rats, administration of CP-91149 in combination with CS-917 suppresses hepatic glycogen reduction by CS-917 and decreases plasma glucose more than single administration of CS-917. [5]
Kinase Assay	Phosphorylase enzyme assay: Human liver glycogen phosphorylase a (HLGPa, 85 ng) activity is measured in the direction of glycogen synthesis by the release of phosphate from glucose-1-phosphate at 22°C in 100 μL of buffer containing 50 mM Hepes (pH 7.2), 100 mM KCl, 2.5 mM EGTA, 2.5 mM MgCl2, 0.5 mM glucose-1-phosphate, and 1 mg/mL glycogen. Phosphate is measured at 620 nm, 20 minutes after the addition of 150 μL of 1 M HCl containing 10 mg/mL ammonium molybdate and 0.38 mg/mL malachite green. Increasing concentrations of CP-91149 are added to the assay in 5 μL of 14% DMSO.
Cell Research	Cells are exposed to various concentrations of CP-91149 for 72hours. Viability is determined with manual cell counts following staining with trypan blue exclusion assay. Cells are fixed with 70% ethanol. DNA is stained with propidium iodide and the intensity of fluorescence is measured using a Becton-Dickinson flow cytometer at 488 nM for excitation and at 650 nM for emission. The cell cycle profile is analyzed using Modifit's Sync Wizard.(Only for Reference)

Molecular Weight	399.87
Formula	C21H22ClN3O3
CAS No.	186392-40-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 74 mg/mL (185.1 mM)

References and Literature

1. Martin WH, et al. Proc Natl Acad Sci U S A, 1998, 95(4), 1776-1781. 2. Aiston S, et al. J Biol Chem, 2001, 276(26), 23858-23866. 3. Schnier JB, et al. Biochem Biophys Res Commun, 2003, 309(1), 126-134. 4. Lerín C, et al. Biochem J. 2004 Mar 15;378(Pt 3):1073-7. 5. Yoshida T, et al. J Pharmacol Sci, 2011, 115(3), 329-335.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library NO PAINS Compound Library Bioactive Compounds Library Max Metabolism Compound Library Bioactive Compound Library Anti-Metabolism Disease Compound Library Anti-Diabetic Compound Library

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H-HomoArg-OH.HCl Ingliforib L-Ascorbic acid 2-phosphate magnesium Calcium glycerophosphate Disodium monofluorophosphate DIPQUO hydrochloride Uric Acid AVE5688

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Keywords

CP-91149 186392-40-5 Metabolism Phosphorylase diabetes CP 91149 A549 NSCLC Inhibitor CP91149 inhibit inhibitor

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