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Licarbazepine (LIC-477D; TRI-477; BIA-2-005; GP-47779) is a novel and potent voltage-gated sodium channel blocker with anticonvulsant, antiepileptic and mood-stabilizing activity. It is an active metabolite of oxcarbazepine and also an enantiomer of licarbazepine.
| ln Vivo |
Eslicarbazepine acetate (ESL) is an oral prodrug that undergoes hydrolytic first-pass metabolism in the liver, which converts it into the physiologically active drug S-licarbazepine quickly and extensively. Prodrug plasma levels continue to be below quantitative thresholds [1]. The main areas of action for the powerful antiepileptic medication ESL are partial seizures and generalized tonic-clonic seizures. Its primary mode of action involves blocking sodium channels that are voltage-gated. Voltage-gated sodium channels, which are crucial for the production and spread of epileptic discharges, are blocked by ESL. When taken orally, ESL is highly absorbed and has a bioavailability that is roughly 16% greater than that of oxcarbazepine (OXC) at an equivalent dosage [1].
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
10-hydroxycarbazepine has known human metabolites that include (2S,3S,4S,5R)-6-[(11-carbamoyl-5,6-dihydrobenzo[b][1]benzazepin-5-yl)oxy]-3,4,5-trihydroxyoxane-2-carboxylic acid. |
| References | |
| Additional Infomation |
Licarbazepine is a dibenzoazepine that is 5H-dibenzo[b,f]azepine, reduced across the C-10,11 positions and carrying a carbamoyl substituent at the azepine nitrogen and a hydroxy function at C-10. A voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects, it is related to oxcarbazepine and is an active metabolite of oxcarbazepine. It has a role as a sodium channel blocker, an anticonvulsant and a drug allergen. It is a carboxamide, a dibenzoazepine and a member of ureas. It is functionally related to a carbamazepine.
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| Molecular Formula |
C15H14N2O2
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|---|---|
| Molecular Weight |
254.289
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| Exact Mass |
254.106
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| CAS # |
29331-92-8
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| Related CAS # |
Licarbazepine-d3;1189917-36-9;Licarbazepine-d4;1020719-39-4;Licarbazepine-d4-1;1188265-49-7
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| PubChem CID |
114709
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| Appearance |
White to off-white solid powder
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| Density |
1.336g/cm3
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| Boiling Point |
431.3ºC at 760mmHg
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| Melting Point |
186-189ºC
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| Flash Point |
214.6ºC
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| Vapour Pressure |
3.33E-08mmHg at 25°C
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| Index of Refraction |
1.677
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| LogP |
3.258
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
19
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| Complexity |
347
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BMPDWHIDQYTSHX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H14N2O2/c16-15(19)17-12-7-3-1-5-10(12)9-14(18)11-6-2-4-8-13(11)17/h1-8,14,18H,9H2,(H2,16,19)
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| Chemical Name |
5-hydroxy-5,6-dihydrobenzo[b][1]benzazepine-11-carboxamide
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| Synonyms |
TRI-477 BIA2-005BIA-2-005 GP47779 LIC477GP-47779 LIC-477 LIC-477D LIC477D TRI477GP-47779 BIA-2-005 Licarbazepine
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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 (~393.27 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.83 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 (9.83 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 25.0 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: ≥ 2.5 mg/mL (9.83 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 | 3.9325 mL | 19.6626 mL | 39.3252 mL | |
| 5 mM | 0.7865 mL | 3.9325 mL | 7.8650 mL | |
| 10 mM | 0.3933 mL | 1.9663 mL | 3.9325 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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