| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
Eslicarbazepine's mechanism of action is as a dual inhibitor of voltage-gated sodium channels and β-secretase (BACE1). It is a cytochrome P450 3A4 inducer and cytochrome P450 2C19 inhibitor. By blocking voltage-gated sodium channels, eslicarbazepine stabilizes the inactivated state of the channel, reducing neuronal excitability and preventing the spread of seizure activity. Its inhibition of β-secretase may have implications for Alzheimer's disease research.
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| ln Vitro |
In vitro, eslicarbazepine has been shown to inhibit voltage-gated sodium channels and β-secretase. Its activity as a sodium channel blocker can be assessed using patch-clamp electrophysiology on neuronal cells. Its inhibition of β-secretase can be assessed using enzyme assays with purified BACE1 enzyme and a fluorogenic substrate.
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| ln Vivo |
Chemically similar to carbamazepine, escicarbazepine is an anti-epileptic medication with a better safety record. Eslicarbazepine acetate serves as a prodrug for eslicarbazepine (S-licarbazepine), a voltage-gated sodium channel and β-secretase dual inhibitor [1][2].
In vivo, eslicarbazepine is used as an oral anticonvulsant for the adjunctive treatment of partial seizures. Eslicarbazepine acetate is a prodrug for eslicarbazepine (S-licarbazepine), which is the active form of the drug. The drug is indicated as a monotherapy or adjunct therapy in the treatment of partial-onset seizures. |
| Enzyme Assay |
Non-cellular enzyme assays for eslicarbazepine involve assessing its inhibition of voltage-gated sodium channels and β-secretase (BACE1). For sodium channel inhibition, purified channel proteins or membrane preparations from brain tissue are used in radioligand binding or electrophysiological assays. For BACE1 inhibition, the enzyme is incubated with a fluorogenic peptide substrate in the presence of varying concentrations of eslicarbazepine, and the cleavage of the substrate is monitored by fluorescence spectroscopy.
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| Cell Assay |
In vitro cellular assays for eslicarbazepine involve treating neuronal cell cultures with the compound and measuring sodium channel currents using patch-clamp electrophysiology. Whole-cell voltage-clamp recordings are performed to assess the inhibition of sodium currents. The compound's effects on neuronal excitability and action potential firing are also assessed. For BACE1 inhibition, cells expressing BACE1 are treated with eslicarbazepine, and the production of Aβ peptides is measured by ELISA.
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| Animal Protocol |
In vivo animal experiments with eslicarbazepine are conducted in rodent models of epilepsy. Seizures are induced using chemical convulsants (e.g., pentylenetetrazole) or electrical stimulation (e.g., maximal electroshock). Animals are treated with eslicarbazepine via oral or intraperitoneal administration, and seizure thresholds, duration, and severity are assessed. The compound's anticonvulsant efficacy and safety profile are evaluated.
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| ADME/Pharmacokinetics |
Eslicarbazepine has a molecular weight of 253.28 and a molecular formula of C₁₅H₁₃N₂O₂. It is a solid powder with a purity of ≥98%. The compound is typically stored at room temperature in a dry, dark place. It is soluble in DMSO and other organic solvents. The compound is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Hepatotoxicity
In premarket clinical trials, it was reported that adding esilicarzepine to standard antiepileptic therapy resulted in a small number of patients experiencing ALT levels exceeding three times the upper limit of normal (ULN) (Probability score: D (likely a rare cause of clinically significant liver injury)). Pregnancy and Lactation Effects ◉ Overview of Use During Lactation There is currently no information regarding the use of esilicarzepine during lactation. However, esilicarzepine is the active metabolite of oxcarbazepine. Limited information suggests that oxcarbazepine is not expected to have any adverse effects on breastfed infants, especially those older than 2 months. Infant lethargy, weight gain, and developmental milestones should be monitored, especially in smaller, exclusively breastfed infants and in combination with other medications. Anticonvulsant ◉ Effects on Breastfed Infants There is currently no specific information on mothers taking esilicarzepine. Please refer to the LactMed record on oxcarbazepine for relevant information. ◉ Effects on lactation and breast milk As of the revision date, no relevant published information was found. Eslicarbazepine is generally well-tolerated at therapeutic doses. Common side effects include dizziness, somnolence, headache, and nausea. It has a more favorable safety profile compared to carbamazepine, with a lower incidence of rash and hyponatremia. The compound should be used with caution in patients with hepatic or renal impairment. Standard safety precautions should be followed when handling the compound. |
| References |
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| Additional Infomation |
(S)-MHD is a dibenzoxazole drug. Eslicarbazepine is an antiepileptic drug, marketed as eslicarbazepine acetate. Eslicarbazepine's mechanism of action is as a cytochrome P450 3A4 inducer and cytochrome P450 2C19 inhibitor. Its physiological effects are achieved by reducing disordered electrical activity in the central nervous system. Eslicarbazepine is an aromatic anticonvulsant, similar to oxcarbazepine, and is often used in combination with other antiepileptic drugs to treat partial seizures. Transient elevations of serum enzymes during eslicarbazepine treatment are rare but have been associated with rare cases of clinically significant liver injury. See also: eslicarbazepine acetate (its active ingredient). The exact mechanism of action of eslicarbazepine is unclear, but it is believed to be related to the inhibition of voltage-gated sodium channels.
Eslicarbazepine (CAS 104746-04-5) is an antiepileptic drug used for the adjunctive treatment of partial-onset seizures. It is a dual inhibitor of voltage-gated sodium channels and β-secretase. Eslicarbazepine is marketed as eslicarbazepine acetate (Aptiom). The compound is chemically related to carbamazepine but has a more favorable safety profile. |
| Molecular Formula |
C15H14N2O2
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| Molecular Weight |
254.289
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| Exact Mass |
254.105
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| CAS # |
104746-04-5
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| PubChem CID |
9881504
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
431.3±55.0 °C at 760 mmHg
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| Melting Point |
188-190°C
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| Flash Point |
214.6±31.5 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.677
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| LogP |
0.93
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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 |
1
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| SMILES |
C1[C@@H](C2=CC=CC=C2N(C3=CC=CC=C31)C(=O)N)O
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| InChi Key |
BMPDWHIDQYTSHX-AWEZNQCLSA-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)/t14-/m0/s1
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| Chemical Name |
(5S)-5-hydroxy-5,6-dihydrobenzo[b][1]benzazepine-11-carboxamide
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| Synonyms |
Erelib EC 810-248-9 BIA 2-194BIA2-194BIA-2194Aptiom Zebinix
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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 : ~250 mg/mL (~983.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.18 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 (8.18 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 20.8 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: ≥ 2.08 mg/mL (8.18 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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