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Ingliforib (CP368296; GPi-296; CP-296; CP-368296) is a novel and potent glycogen phosphorylase inhibitor with cardioprotective activity.. It exhibits IC50s of 52, 352 and 150 nM for liver, muscle and brain glycogen phosphorylase. Glycogen phosphorylase is the rate-limiting enzyme in glycogenolysis, thereby Ingliforib can prevent the release of glucose-1 phosphate from a glycogen molecule in liver. It also inhibits glycogen phosphorylase in cardiac muscle and thus protects the heart from myocardial ischemic injury by preserving glycogen content and improving glycolytic-oxidative coupling.
| ln Vitro |
Glycogen phosphorylase inhibitor ingliforib has IC50 values of 352 and 150 nM, respectively, for the cardiac GP isoforms (muscle and brain), and it has a substantial inhibitory effect on the hepatic isoform (IC 50 of 52 nM). In isolated rabbit hearts, ingliforib (0.1, 1, 10 μM) lowers infarct size in a dose-dependent manner [1].
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| ln Vivo |
In rabbits undergoing thoracotomy anesthesia, ingliforib (15 mg/kg) substantially decreased infarct size by 52% and decreased plasma glucose and lactate concentrations. In anesthetized rabbits, ingliforib (15 mg/kg) also suppresses the activity of total glycogen phosphorylase (GP) and cardiac glycogen phosphorylase a (GPa) [1].
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| Animal Protocol |
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| References |
[1]. Tracey WR, et al. Cardioprotective effects of ingliforib, a novel glycogen phosphorylase inhibitor. Am J Physiol Heart Circ Physiol. 2004 Mar;286(3):H1177-84
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| Additional Infomation |
Ingliforib is an indolecarboxamide.
Ingliforib is a glycogen phosphorylase inhibitor with antihyperglycemic and cardioprotective activities. Ingliforib inhibits glycogen phosphorylase, the rate-limiting enzyme in glycogenolysis, thereby preventing the release of glucose-1 phosphate from a glycogen molecule in liver. This agent also inhibits glycogen phosphorylase in cardiac muscle and may protect the heart from myocardial ischemic injury by preserving glycogen content and improving glycolytic-oxidative coupling. |
| Molecular Formula |
C23H24CLN3O5
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|---|---|
| Molecular Weight |
457.91
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| Exact Mass |
457.14
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| CAS # |
186392-65-4
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| PubChem CID |
6451325
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.495g/cm3
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| Boiling Point |
843.3ºC at 760 mmHg
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| Flash Point |
463.8ºC
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| Vapour Pressure |
3.31E-30mmHg at 25°C
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| Index of Refraction |
1.712
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
666
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| Defined Atom Stereocenter Count |
4
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| SMILES |
ClC1C([H])=C([H])C2=C(C=1[H])C([H])=C(C(N([H])[C@@]([H])(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])[C@]([H])(C(N1C([H])([H])[C@]([H])([C@]([H])(C1([H])[H])O[H])O[H])=O)O[H])=O)N2[H]
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| InChi Key |
GVDRRZOORHCTAN-MJUUVYJYSA-N
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| InChi Code |
InChI=1S/C23H24ClN3O5/c24-15-6-7-16-14(9-15)10-18(25-16)22(31)26-17(8-13-4-2-1-3-5-13)21(30)23(32)27-11-19(28)20(29)12-27/h1-7,9-10,17,19-21,25,28-30H,8,11-12H2,(H,26,31)/t17-,19-,20+,21+/m0/s1
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| Chemical Name |
(R-(R*,S*-(cis)))-5-Chloro-N-(3-(3,4-dihydroxy-1-pyrrolidinyl)-2-hydroxy-3-oxo-1-(phenylmethyl)propyl)-1H-indole-2-carboxamide
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| Synonyms |
Ingliforib CP 296 GPi-296CP-368296GPi296CP-368 CP-296CP 296 CP368296CP296 CP368 CP 368,296 CP 368296.
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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 : ~130 mg/mL (~283.90 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (4.74 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 21.7 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: ≥ 2.17 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 21.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1838 mL | 10.9192 mL | 21.8384 mL | |
| 5 mM | 0.4368 mL | 2.1838 mL | 4.3677 mL | |
| 10 mM | 0.2184 mL | 1.0919 mL | 2.1838 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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