Lamotrigine
Based on 7 publication(s) in Google Scholar
Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.97%
- No. CAS: 84057-84-1
- Fòrmula: C9H7Cl2N5
- Peso molecular:256.09
-
Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Anti-COVID-19 Compound Library
HY-L052
-
NMPA-Approved Drug Library
HY-L053
-
Orally Active Compound Library
HY-L061
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Neuroprotective Compound Library
HY-L070
-
Drug-Induced Liver Injury (DILI) Compound Library
HY-L076
-
Mechanoreceptors Compound Library
HY-L095
-
Rare Diseases Drug Library
HY-L102
-
Pediatric Drug Library
HY-L104
-
Sodium Channel Blocker Library
HY-L118
-
FDA-Approved Anticancer Drug Library
HY-L122
-
Human Metabolite Library
HY-L123
-
Anti-Aging Natural Product Library
HY-L134
-
Off-patent Drug Library
HY-L141
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Ion Channel Compound Library
HY-L166
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Nephrotoxicity Compound Library
HY-L229
-
RNA Binding Bioactive Compound Library
HY-L248
-
Classic FDA-Approved Drug Library
HY-L261
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
FDA-Approved Drug Library
HY-L022
-
Anti-Cancer Compound Library
HY-L025
-
CNS-Penetrant Compound Library
HY-L028
-
Autophagy Compound Library
HY-L029
-
Drug Repurposing Compound Library
HY-L035
Publications Citing Use of MedChemExpress (MCE) Lamotrigine
More- Nat Chem Biol. 2025 Jun 2. [Abstract]
- Proc Natl Acad Sci U S A. 2023 Oct 10;120(41):e2309773120. [Abstract]
- JCI Insight. 2022 Aug 8;7(15):e160247. [Abstract]
- Cell Calcium. 2022 Mar:102:102527. [Abstract]
- Pharmacol Res Perspect. 2021 Oct;9(5):e00879. [Abstract]
- Pharmacol Res Perspect. 2020 Apr;8(2):e00575. [Abstract]
- Pharmacol Biochem Behav. 2018 May:168:43-50. [Abstract]
Customer Validation & Images
-
In Vivo Efficacy Study
-
In Vivo Efficacy Study
-
In Vivo Efficacy Study
-
In Vivo Efficacy Study
-
Cell Proliferation/Viability Assay
Actividad biológica
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>100 μM
Compound: 23
|
Inhibition of human Nav1.2 channel expressed in HEK cells by patch-clamp electrophysiology method
Inhibition of human Nav1.2 channel expressed in HEK cells by patch-clamp electrophysiology method
|
[PMID: 19394229] |
| HEK293 | IC50 |
10 μM
Compound: Lamotrigine
|
Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp technique
Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp technique
|
[PMID: 18501613] |
| HEK293 | IC50 |
62 μM
Compound: Lamotrigine
|
Inhibition of human recombinant Nav1.5 channel expressed in HEK293 cells by whole cell voltage clamp technique
Inhibition of human recombinant Nav1.5 channel expressed in HEK293 cells by whole cell voltage clamp technique
|
[PMID: 18501613] |
| HEK293 | IC50 |
96 μM
Compound: Lamotrigine
|
Inhibition of human recombinant Nav1.8 channel expressed in HEK293 cells by whole cell voltage clamp technique
Inhibition of human recombinant Nav1.8 channel expressed in HEK293 cells by whole cell voltage clamp technique
|
[PMID: 18501613] |
| HEK293 | IC50 |
98 μM
Compound: lamotrigine
|
Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
|
[PMID: 26101568] |
| Oocyte | IC50 |
8.1 μM
Compound: 9, LTG
|
Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes
Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes
|
[PMID: 18178093] |
| SH-SY5Y | IC50 |
17 μM
Compound: lamotrigine
|
Inhibition of human Nav1.2 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
Inhibition of human Nav1.2 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
|
[PMID: 26101568] |
| SH-SY5Y | IC50 |
17 μM
Compound: lamotrigine
|
Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
|
[PMID: 26101568] |
| SH-SY5Y | IC50 |
17 μM
Compound: lamotrigine
|
Inhibition of human Nav1.7 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
Inhibition of human Nav1.7 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
|
[PMID: 26101568] |
Lamotrigine inhibits Veratrine evoked release of glutamate and aspartate with ED50 values of 21 μM for both amino acids, but Lamotrigine is less potent in the inhibition of GABA release (ED50=44 μM. At concentrations up to 300 μM, LTG has no effect on patassium-evoked amino acid[1].? Lamotrigine is some five times less potent in the inhibition of Veratrine-evoked [3H]acetylcholine release (ED50=100 μM) than in glutamate or aspartate release[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:White male mice weighing 25-30 g[2]
-
Dosage:10 mg/kg, 15 mg/kg or 20 mg/kg
-
Administration:Intraperitoneally 30 min before pentylenetetrazol
-
Result:Had an anti-convulsive effect in seizure models, suppressing seizure intensity and influencing the latency to the first seizure.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 84057-84-1
-
Appearance Solid
-
Peso molecular 256.09
-
Fòrmula C9H7Cl2N5
-
Color White to off-white
-
SMILES
NC1=NC(N)=C(C2=CC=CC(Cl)=C2Cl)N=N1
-
Synonyms
LTG; BW430C
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (7)
-
Journal Impact Factor
-
Most Recent
-
Nat Chem Biol
2025 Jun 2. PMID: 40456963 -
Proc Natl Acad Sci U S A
2023 Oct 10;120(41):e2309773120. PMID: 37782796 -
JCI Insight
Pharmacological induction of AMFR increases functional EAAT2 oligomer levels and reduces epileptic seizures in mice. [Abstract]2022 Aug 8;7(15):e160247. PMID: 35938532
Lamotrigine purchased from MedChemExpress. Usage Cited in: JCI Insight. 2022 Aug 8;7(15):e160247. [Abstract]
Mice were administered Lamotrigine (20 mg/kg) or vehicle 1 hour before PTZ injections. Pretreatment with the positive control Lamotrigine (LTG) significantly decreased the severity of acute seizures.
Lamotrigine purchased from MedChemExpress. Usage Cited in: JCI Insight. 2022 Aug 8;7(15):e160247. [Abstract]
Mice were administered Lamotrigine (20 mg/kg) or vehicle 1 hour before PTZ injections. Mice in the Lamotrigine group showed a delayed response to PTZ.
Lamotrigine purchased from MedChemExpress. Usage Cited in: JCI Insight. 2022 Aug 8;7(15):e160247. [Abstract]
Examples of daily recordings of spontaneous recurrent seizures in the vehicle, Lamotrigine, APAP and APAP/17AAG treatment groups. Lamotrigine was administered i.p. at a dose of 20 mg/kg daily.
Lamotrigine purchased from MedChemExpress. Usage Cited in: JCI Insight. 2022 Aug 8;7(15):e160247. [Abstract]
The intrahippocampal injection of KA reliably models refractory TLE with HS and the model mice displayed drug-resistant characteristics after repeated administration of Lamotrigine.
-
Cell Calcium
Mutations and clinical significance of calcium voltage-gated channel subunit alpha 1E (CACNA1E) in non-small cell lung cancer. [Abstract]2022 Mar:102:102527. PMID: 35026540
Lamotrigine purchased from MedChemExpress. Usage Cited in: Cell Calcium. 2022 Mar:102:102527. [Abstract]
The cells were treated with Lamotrigine (0-150 μM) at indicated concentrations for 48 h and analyzed by CCK-8 Cell Counting assay.
Lamotrigine purchased from MedChemExpress. Usage Cited in: Cell Calcium. 2022 Mar:102:102527. [Abstract]
Effects of Lamotrigine (0-25 μM) on colony forming activity of H1299 and H1975 cells.
-
Pharmacol Res Perspect
Effects of membrane transport activity and cell metabolism on the unbound drug concentrations in the skeletal muscle and liver of drugs: A microdialysis study in rats. [Abstract]2021 Oct;9(5):e00879. PMID: 34628723 -
Pharmacol Res Perspect
Applicability of free drug hypothesis to drugs with good membrane permeability that are not efflux transporter substrates: A microdialysis study in rats. [Abstract]2020 Apr;8(2):e00575. PMID: 32266794 -
Pharmacol Biochem Behav
Anticonvulsants lamotrigine and riluzole disrupt maternal behavior in postpartum female rats. [Abstract]2018 May:168:43-50. PMID: 29572014
Solvente y solubilidad
DMSO : 25 mg/mL (97.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (39.05 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (278 KB)
-
SDS (645 KB)
- English - EN (645 KB)
- Français - FR (645 KB)
- Deutsch - DE (645 KB)
- Norwegian - NO (645 KB)
- Español - ES (645 KB)
- Swedish - SV (645 KB)
- Italian - IT (645 KB)
- Korean - KR (645 KB)
- Portuguese - PT (645 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. M J Leach, et al. Pharmacological studies on lamotrigine, a novel potential antiepileptic drug: II. Neurochemical studies on the mechanism of action. Epilepsia. Sep-Oct 1986;27(5):490-7. [Content Brief]
[2]. Damianka P Getova, et al. A study of the effects of lamotrigine on mice using two convulsive tests. Folia Med (Plovdiv). Apr-Jun 2011;53(2):57-62. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.9049 mL | 19.5244 mL | 39.0488 mL | 97.6219 mL |
| 5 mM | 0.7810 mL | 3.9049 mL | 7.8098 mL | 19.5244 mL | |
| 10 mM | 0.3905 mL | 1.9524 mL | 3.9049 mL | 9.7622 mL | |
| 15 mM | 0.2603 mL | 1.3016 mL | 2.6033 mL | 6.5081 mL | |
| 20 mM | 0.1952 mL | 0.9762 mL | 1.9524 mL | 4.8811 mL | |
| 25 mM | 0.1562 mL | 0.7810 mL | 1.5620 mL | 3.9049 mL | |
| 30 mM | 0.1302 mL | 0.6508 mL | 1.3016 mL | 3.2541 mL | |
| 40 mM | 0.0976 mL | 0.4881 mL | 0.9762 mL | 2.4405 mL | |
| 50 mM | 0.0781 mL | 0.3905 mL | 0.7810 mL | 1.9524 mL | |
| 60 mM | 0.0651 mL | 0.3254 mL | 0.6508 mL | 1.6270 mL | |
| 80 mM | 0.0488 mL | 0.2441 mL | 0.4881 mL | 1.2203 mL |
Lamotrigine Related Classifications
HY-B0495 Related Classifications
Powered by Bioz