Lamotrigine - Moligand™, 10mM in DMSO , Sodium channel alpha subunit blocker, CAS No.84057-84-1, Sodium channel alpha subunit blocker

CAS: 84057-84-1 Cat. No.: L409197 Molecular Weight: 256.09 EC Number: 281-901-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

BW-430C | 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Lamotrigine Lamotrigine (BW-430C) 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.
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, 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 . Lamotrigine inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels. 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.

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. 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.
Cell Data

cell lines：Murine cortical neurons and cerebellar granule cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

BW-430C | 6-(2, 3-dichlorophenyl)-1, 2, 4-triazine-3, 5-diamine

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Lamotrigine (BW-430C) 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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

BLOCKER, CHANNEL BLOCKER

Mechanism of action

Sodium channel alpha subunit blocker

Product Properties

• ALogP: 1.4

Names and Identifiers

• Isomeric SMILES: C1=CC(=C(C(=C1)Cl)Cl)C2=C(N=C(N=N2)N)N
• WGK Germany: 3
• RTECS: XY5850700
• Molecular Weight: 256.09
• Reaxy-Rn: 7589268
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7589268&ln=

Associated Targets(Human)

SCN2A Tclin Sodium channel protein type 2 subunit alpha (2 Activities)

Discover Target: SCN2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Melt Point(°C): 216-218°C

References

1. Rong Wang, Tianfeng Wan, Wenqing Li, Zilin Chen.  (2021)  Schiff base network-1 incorporated monolithic column for in-tube solid phase microextraction of antiepileptic drugs in human plasma.  TALANTA,      [PMID:33676655] [10.1016/j.talanta.2021.122098]

2. Lanteng Wang, Jin Wang, Ang Zhang, Xin-an Huang, Hongtao Lei.  (2021)  Two binding epitopes modulating specificity of immunoassay for β-agonist detection: Quantitative structure–activity relationship.  FOOD CHEMISTRY,      [PMID:34537613] [10.1016/j.foodchem.2021.131071]

3. Qin Zhou, Yishi Wei, Yijing Liao, Xing Hu, Deming Gong, Guowen Zhang.  (2024)  Inhibitory mechanism of α-glucosidase by liquiritigenin and its combined effect with acarbose: Multi-spectroscopic analyses and molecular docking simulation.  Food Bioscience,      [PMID:] [10.1016/j.fbio.2024.105659]