Art. -Nr.: HY-B0495

Lamotrigine

(Synonyms: LTG; BW430C)

7 Cited Publications

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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.

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Reinheit: 99.97%
CAS. Nr.: 84057-84-1
Formel: C₉H₇Cl₂N₅
Molecular Weight:256.09

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lamotrigine Chemical Structure

CAS. Nr.: 84057-84-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

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]

In Vitro

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.

In Vivo

Lamotrigine (IP, 30 min before pentylenetetrazol; 10 mg/kg, 15 mg/kg or 20 mg/kg) decreases the seizure intensity?at the higher doses, it increases the latency to the first pentylenetetrazol-induced seizure?in all studied doses compared with the controls^[2].

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 84057-84-1
Appearance Solid
Molecular Weight 256.09
Formel C₉H₇Cl₂N₅
Color White to off-white
SMILES

NC1=NC(N)=C(C2=CC=CC(Cl)=C2Cl)N=N1
Synonyms

LTG; BW430C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (7)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayCell Imaging/Staining

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Journal Impact Factor

Nat Chem Biol

Pharmacological inhibition of PSPH reduces serine levels and epileptic seizures. [Abstract]

2025 Jun 2. PMID: 40456963
Proc Natl Acad Sci U S A

Dual-pocket inhibition of Nav channels by the antiepileptic drug lamotrigine. [Abstract]

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.9049 mL

19.5244 mL

39.0488 mL

5 mM

0.7810 mL

3.9049 mL

7.8098 mL

10 mM

0.3905 mL

1.9524 mL

3.9049 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (9.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (39.05 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Lamotrigine

7 Cited Publications

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Lamotrigine

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Publications Citing Use of MedChemExpress (MCE) Lamotrigine

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lamotrigine Related Classifications

HY-B0495 Related Classifications