| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Purity: ≥98%
CP 91,149 is a novel, potent and selective inhibitor of human liver glycogen phosphorylase a (LGPa) with IC50 of 0.13 μM in the presence of glucose, 5- to 10-fold less potent in the absence of glucose. It also inhibits muscle glycogen phosphorylase a (MGPa), and MGPb (IC50s = 0.13, 0.2, and 0.3 μM, respectively, in the presence of glucose. CP 91,149 is 5- to 10-fold less potent in the absence of glucose. In vitro, it inhibits glucagon-stimulated glycogenolysis in primary human hepatocytes (IC50 = 2.1 μM) and increases glycogen synthesis in rat hepatocytes at a concentration of 2.5 μM in the presence of 5 mM glucose. CP 91,149 inhibits brain GP (IC50 = 0.5 μM) and, at a concentration of 30 μM, inhibits glycogen accumulation and proliferation of A549 non-small cell lung carcinoma (NSCLC) cells that express endogenous brain GP. In vivo, CP 91,149 (25 mg/kg, p.o.) lowers the plasma glucose level in diabetic ob/ob mice within 3 hours of administration without producing hypoglycemia, but has no effect on normoglycemic, non-diabetic mice. 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.
| ln Vitro |
By blocking AMP-mediated GP b activation and converting the phosphorylated AMP-independent α form of muscle GP activity to the dephosphorylated AMP-dependent b form, CP-91149 therapy lowers muscle GP activity [1]. In A549 cells, CP-91149 (10, 30, 50 μM) inhibits brain GP and results in a buildup of glycogen [2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Cells were transduced with adenovirus and incubated in the presence of 25 mM glucose for 2 days. Tested Concentrations: 10 µM (glucose− or glucose+ for 18 hrs (hours)). Incubation Duration: 3 hrs (hours). Experimental Results: Conversion of GP a to GP b was promoted according to the proposed α model in hepatocytes. Western Blot Analysis[2] Cell Types: A549 cells. Tested Concentrations: 0, 10, 30, 50 μM. Incubation Duration: 72 hrs (hours). Experimental Results: A significant increase in glycogen accumulation was detected with 10 μM CP-91149 compared to untreated cells (maximum glycogen accumulation was 30 μM). At a concentration of 50 μM CP-91149, intracellular glycogen content was diminished, which may be due to other pharmacological effects of the drug. CP-91149 Dose-dependent accumulation of intracellular glycogen in A549 cells indicates that CP-91149 inhibits brain GP in tissue culture. |
| References |
European journal of biochemistry / FEBS. 2003;270(13):2773-2781; Proceedings of the National Academy of Sciences of the United States of America. 1998;95(4):1776-1781.
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| Molecular Formula |
C21H22N3O3CL
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|---|---|
| Molecular Weight |
399.87068
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| Exact Mass |
399.135
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| CAS # |
186392-40-5
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| PubChem CID |
9843900
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| Appearance |
White to off-white solid powder
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| Melting Point |
190-192°C
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| LogP |
3.186
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
553
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CN(C)C(=O)[C@@H]([C@H](CC1=CC=CC=C1)NC(=O)C2=CC3=C(N2)C=CC(=C3)Cl)O
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| InChi Key |
HINJNZFCMLSBCI-PKOBYXMFSA-N
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| InChi Code |
InChI=1S/C21H22ClN3O3/c1-25(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 |
1H-Indole-2-carboxamide, 5-chloro-N-((1S,2R)-3-(dimethylamino)-2-hydroxy-3-oxo-1-(phenylmethyl)propyl)-
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| Synonyms |
CP-91149; CP 91149; CP91149; UNII-O8EV00W45A.
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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 : ~100 mg/mL (~250.08 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.25 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 25.0 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: ≥ 2.5 mg/mL (6.25 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 25.0 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 | 2.5008 mL | 12.5041 mL | 25.0081 mL | |
| 5 mM | 0.5002 mL | 2.5008 mL | 5.0016 mL | |
| 10 mM | 0.2501 mL | 1.2504 mL | 2.5008 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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