Lamotrigine

Catalog No.S3024

Lamotrigine 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 also is a sodium channel blocker.

Price Stock Quantity  
In DMSO USD 120 In stock
USD 90 In stock
USD 270 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Lamotrigine Chemical Structure

Lamotrigine Chemical Structure
Molecular Weight: 256.09

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Lamotrigine is available in the following compound libraries:

Product Information

  • Compare Sodium Channel Chemicals
    Compare Sodium Channel Products
  • Research Area

Product Description

Biological Activity

Description Lamotrigine 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 also is a sodium channel blocker.
Targets Sodium channel [1]
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. [1] In rat cerebral cortex tissue incubated with veratrine 10 mg/L, lamotrigine 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 . [2]Lamotrigine inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels. [3] Lamotrigine 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. [4]
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 lamotrigine administration and persist for more than 24 hours. [4] Lamotrigine 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 lamotrigine in rats at intravenous doses >5 mg/kg. [5]
Features

Protocol(Only for Reference)

Kinase Assay: [3]

Electrophysiology In electrophysiological experiments, neurons bathed in control medium responds to 500-ms depolarizing pulses with trains of action potentials termed sustained repetitive firing (SRF). Increasing the magnitude of depolarization results in an increased number and frequency of action potentials. Typically a depolarizing current step of l-l.5 nA is sufficient to evoke SRF. To test the anticonvulsant effect, the blocking of SRF throughout the depolarizing current pulse is analyzed.

Animal Study: [3]

Animal Models Dog/Rat
Formulation suspended in 0.25% methylcellulose solution
Dosages 4.5 and 11.7 mg /kg in dogs and rats, respectively
Administration i.v.
Solubility 0.5% methylcellulose, , 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
1

References

[1] Goa KL, et al. Drugs, 1993, 46(1), 152-176.

[2] Leach MJ, et al. Epilepsia, 1986, 27(5), 490-497.

view more

Chemical Information

Download Lamotrigine SDF
Molecular Weight (MW) 256.09
Formula

C9H7Cl2N5

CAS No. 84057-84-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 10 mg/mL (39 mM)
Water <1 mg/mL (<1 mM)
Ethanol 3 mg/mL (11 mM)
In vivo 0.5% methylcellulose, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine

Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Sodium Channel Products

  • Selinexor (KPT-330)

    Selinexor (KPT-330) is an orally bioavailable selective CRM1 inhibitor. Phase 2.

  • KPT-185

    KPT-185 is a selective CRM1 inhibitor.

  • CFTRinh-172

    CFTRinh-172 is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters.

  • Riluzole

    Riluzole is a drug used to treat amyotrophic lateral sclerosis.

  • Rufinamide

    Rufinamide, a triazole derivative, is an anticonvulsant medication.

  • Amiloride HCl dihydrate

    Amiloride HCl dihydrate is a potent epithelial sodium channel blocker.

  • A-803467

    A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.

    Features:The 1st small-molecule blocker of sodium channels showing both high potency and significant subtype-selectivity among the sodium channel family.

  • Ouabain

    Ouabain is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM.

    Features:A glycoside poison that binds to and inhibits the action of the Na+/K+ pump in the cell membrane.

  • Vinpocetine

    Vinpocetine is a selectively inhibitor of voltage-sensitive sodium channel for the treatment of stroke, vascular dementia and Alzheimer's disease.

  • Propafenone HCl

    Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.

Recently Viewed Items

Tags: buy Lamotrigine | Lamotrigine ic50 | Lamotrigine price | Lamotrigine cost | Lamotrigine solubility dmso | Lamotrigine purchase | Lamotrigine manufacturer | Lamotrigine research buy | Lamotrigine order | Lamotrigine mouse | Lamotrigine chemical structure | Lamotrigine mw | Lamotrigine molecular weight | Lamotrigine datasheet | Lamotrigine supplier | Lamotrigine in vitro | Lamotrigine cell line | Lamotrigine concentration | Lamotrigine nmr
Contact Us