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Lamotrigine Sodium Channel inhibitor

Name: Lamotrigine
Brand: Selleck Chemicals
SKU: S3024
Availability: InStock
Rating: 5 (13 reviews)

Cat.No.S3024

Lamotrigine (BW-430C,LTG) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and this compound also is a sodium channel blocker.

Chemical Structure

Molecular Weight: 256.09

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Quality Control

Batch: S302401 DMSO]10 mg/mL]false]Ethanol]3 mg/mL]false]Water]Insoluble]false Purity: 99.76%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.76

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Other Sodium Channel Inhibitors	Camostat Mesilate A-803467 cariporide Veratramine Bulleyaconi cine A Vinpocetine Tenapanor PF-06869206 Sparteine (-)-Sparteine Sulfate

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (39.04 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	0.5% methylcellulose Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (39.05mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	256.09	Formula	C₉H₇Cl₂N₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	84057-84-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BW-430C,LTG			Smiles	C1=CC(=C(C(=C1)Cl)Cl)C2=C(N=C(N=N2)N)N

Mechanism of Action

Targets/IC₅₀/Ki	Sodium channel 5-HT (human platelets) 240 μM 5-HT (rat brain synaptosomes) 474 μM
In vitro	Lamotrigine stabilises presynaptic neuronal membranes by blockade of voltage-dependent sodium channels, thus preventing the release of excitatory neurotransmitters, particularly glutamate and aspartate. In rat cerebral cortex tissue incubated with veratrine 10 mg/L, this compound is twice as potent in inhibiting the release of glutamate and aspartate (ED 50 = 5.38 mg/L for each) than the release of GABA (ED50 = 11.2 mg/L), and is much less potent in inhibiting acetylcholine release (ED50 = 25.6 mg/L) when cortical slices is exposed to veratrine 75 mg/L. Basal glutamate release is unaffected . This chemical inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels. It does not induce PCP-like central nervous system (CNS) effects, does not act by direct inhibition at the NMDA receptor, and would be expected to be devoid of the undesirable effects associated with NMDA blockade.
In vivo	In mice and rats, lamotrigine prevents MES- and pentetrazol-induced hindlimb extension, suggesting an antiepileptic profile in animals. These effects peak 1 hour after this compound administration and persist for more than 24 hours. This chemical is active in the electrically evoked EEG after-discharge test, which is thought to indicate activity against both simple and complex partial seizures. After-discharge duration is reduced dose-dependently by this compound in rats at intravenous doses >5 mg/kg.
References	[1] https://pubmed.ncbi.nlm.nih.gov/7691504/ [2] https://pubmed.ncbi.nlm.nih.gov/3757936/ [3] https://pubmed.ncbi.nlm.nih.gov/1334455/ [4] https://pubmed.ncbi.nlm.nih.gov/3757935/ [5] https://pubmed.ncbi.nlm.nih.gov/2492222/ [6] http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=d7e3572d-56fe-4727-2bb4-013ccca22678#nlm34090-1

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06049095	Recruiting	Healthy	Latigo Biotherapeutics	October 17 2023	Phase 1
NCT05420350	Recruiting	Meniere Disease\|Ménière''s Vertigo\|Vertigo Intermittent\|Vertigo Aural	Dent Neuroscience Research Center\|Cures Within Reach\|Dent Family Foundation	December 16 2020	Phase 2

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