计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 3 篇同行评审文献引用。
概述
Lamotrigine是一种新型抗惊厥药剂，作用于人类血小板和大鼠脑突触体，抑制5-羟色胺(5-HT)吸收，IC50分别为240 μM和474 μM。A sodium channel protein inhibitor.
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%
规格
英文别名
BW-430C | 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Lamotrigine
生化机理
拉莫三嗪（BW-430C）是一种新型抗惊厥药物，在人血小板和大鼠脑突触体中抑制 5-HT 的 IC50 值分别为 240 μM 和 474 μM，同时也是一种钠通道阻滞剂。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
封闭剂
作用机制
钠通道α亚基阻断剂
名称和识别符
EC号
281-901-8
分子类型
小分子
Isomeric SMILES
C1=CC(=C(C(=C1)Cl)Cl)C2=C(N=C(N=N2)N)N
分子量
256.09
Reaxy-Rn
7589268
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7589268&ln=
技术文档
高级数据
产品属性
| ALogP | 1.4 |
|---|
关联靶点（人）
SCN2A
Tclin
钠通道蛋白 2 型亚基 α(Sodium channel protein type 2 subunit alpha)
(2 活性数据)
化学和物理性质
熔点
216-218°C
安全和危险性（GHS）
象形图
信号词
Danger
危险声明
H301: 吞咽会中毒
预防措施声明
P321: 特殊处理（请参阅此标签上的...）。
P405: 密闭存放
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P301+P316: 如果吞咽：立即寻求紧急医疗救助。
WGK Germany
3
RTECS
XY5850700
Merck Index
5353
个人防护装备
Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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危险品化学品经营许可证（带存储）