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Lamotrigine/拉莫三嗪 {[allProObj[0].p_purity_real_show]}

货号:A551325 同义名: LTG; BW430C

Lamotrigine 是一种抗癫痫化合物,能够阻断钠离子通道,并且对L型、N型和P型钙通道有抑制作用。它对5-HT3受体具有弱抑制作用,IC50值为240 μM(血小板)和474 μM(大鼠脑)。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Lamotrigine/拉莫三嗪 化学结构 CAS号:84057-84-1
Lamotrigine/拉莫三嗪 化学结构
CAS号:84057-84-1
Lamotrigine/拉莫三嗪 3D分子结构
CAS号:84057-84-1
Lamotrigine/拉莫三嗪 化学结构 CAS号:84057-84-1
Lamotrigine/拉莫三嗪 3D分子结构 CAS号:84057-84-1
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Lamotrigine/拉莫三嗪 纯度/质量文件 产品仅供科研

货号:A551325 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Ca2+ channel-like protein Calcium Channel Cav 2.2 其他靶点 纯度
CDC25B-IN-2 Akt 99%+
Clevidipine 97%
Verapamil HCl 99%
Amlodipine 99%
Amlodipine maleate 98%
(+)-cis-Diltiazem HCl 99%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

99%+
Tanshinone IIA sulfonate sodium 98%
Ulixacaltamide ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

99%+
Dronedarone HCl 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

98%
Efonidipine HCl monoethanolate 98%
Cinnarizine 98%
SEA0400 ++

NCX, IC50: 33 nM

ERK,ROS,p38 MAPK 99%+
Fasudil HCl Rho,PKA 98%
ML-9 MLCK,Akt 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

95%
Lomerizine 2HCl 98%
Efonidipine 98%
Levamlodipine 98%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

97%
Isradipine 98%
Lacidipine 98%
Lercanidipine 99%
Loureirin B Potassium Channel 99%+
Tetracaine HCl 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

99%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

98%
Nicardipine 99%
Wilforgine 98+%
Econazole 99%+
Ginsenoside Rd NF-κB 98%
Fendiline HCl 98+%
Mesaconitine 98%
Tetrandrine 95%
Nifedipine 98%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

95%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

95+%
Azelnidipine 97%
Levetiracetam 98%
Nimodipine 95%
Benidipine HCl 98%
Pinaverium bromide 98%
Pranidipine 99%
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

95%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

97%
Cilnidipine 99%
Cinepazide Maleate 99% (HPLC)
Terfenadine 98%
YM-58483 99%+
Amiloride HCl 98%
Ranolazine 98%
Praeruptorin A Akt,p38 MAPK 98%
Ranolazine 2HCl 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

98%
Levamlodipine besylate 97%
Carboxyamidotriazole Orotate 98%
IGS-1.76 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

++++

Cav 2.2, IC50: 0.001 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Sodium Channel 其他靶点 纯度
Tolperisone HCl 99%
Triamterene +++

ENaC, IC50: 4.5 μM

98%
Lamotrigine 98%
Vinpocetine 98%
Zonisamide 99%
Dronedarone HCl 95%
Procainamide HCl 99%
Bupivacaine HCl 99+%
Benzocaine 98%
Carbamazepine ++

Sodium channel, IC50: 131 μM

98%
Quinidine sulfate dihydrate 98%
Ibutilide fumarate 99%+
Dibucaine HCl 99+%
Mexiletine HCl 99%
Phenytoin 99+%
Camostat Mesylate +++

epithelial sodium channel (ENaC), IC50: 50 nM

99%+
Levobupivacaine 97+%
Oxcarbazepine +

sodium channel, IC50: 160 μM

98%
Amiloride HCl dihydrate 97%
Ambroxol 98+%
Primidone 99%
Propafenone 99%
A-803467 ++++

Na(V1.8) channel, IC50: 8 nM

99%+
Rufinamide 99%
Phenytoin sodium 98%
Proparacaine HCl +

Voltage-gated sodium channel, ED50: 3.4 mM

98+%
Amiloride HCl 98%
Riluzole 97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Lamotrigine/拉莫三嗪 生物活性

靶点
  • 5-HT

    5-HT (rat brain synaptosomes), IC50:474 μM

    5-HT (human platelets), IC50:240 μM

  • Sodium Channel

描述 Lamotrigine belongs to the second generation of antiepileptic drugs (AEDs)[3]. Co-application of lamotrigine (1 ~ 300 µM) resulted in a concentration-dependent reduction in peak amplitude of currents induced by 3 µM of 5-HT for an IC50 value of 28.2 ± 3.6 µM with a Hill coefficient of 1.2 ± 0.1[4]. Moreover, intrathecally administered lamotrigine could prevent the activation of the glutamate receptors involved in pain transmission and central sensitization, such as AMPA, NMDA, and metabotropic receptors[5]. Studies showed lamotrigine could ameliorate executive dysfunction and brain inflammatory response in the mouse model of AD[6].

Lamotrigine/拉莫三嗪 细胞实验

Cell Line
Concentration Treated Time Description References
Retinal Ganglion Cells (RGCs) 200 µM 3 min Lamotrigine reduced the firing rates in Nf1+/neoRGC neurons (>80% decrease), indicating that HCN channel activation attenuates neuronal excitability. Nat Commun. 2022 May 19;13(1):2785.
tsA201 cells 200 μM 3 min Lamotrigine exhibited significantly greater tonic block of Na V1.1-5N channels compared to Na V1.1-5A channels. Epilepsia. 2011 May;52(5):1000-9.
NT2-N cells 50 µM 24 h To investigate the effects of lamotrigine on mRNA-lncRNA co-expression patterns in NT2-N cells, revealing the complex mechanisms of bipolar disorder drugs. Front Pharmacol. 2022 Apr 8;13:873271.
C8-B4 cells 0.05 mM 24 h To evaluate the effect of lamotrigine on the release of inflammatory cytokines in LPS-stimulated C8-B4 cells. Results showed that lamotrigine alone had minor effects on cytokine release, but when combined with quetiapine, it significantly reduced cytokine release, indicating an anti-inflammatory effect. Int J Neuropsychopharmacol. 2018 Jun 1;21(6):582-591.
NT2-N cells 0.05 mM 24 h To evaluate the effect of lamotrigine on the expression of mitochondrial function genes in NT2-N cells. Results showed that lamotrigine significantly increased the expression of PGC1α, indicating a promotion of mitochondrial biogenesis. Int J Neuropsychopharmacol. 2018 Jun 1;21(6):582-591.
NT2-N cells 50 µM 24 h To assess the effects of lamotrigine on ribosomal gene expression, results showed that lamotrigine significantly downregulated ribosomal gene expression, but the effect was no longer significant when the p-value was adjusted as a q-value to account for false discovery rate (FDR). Int J Mol Sci. 2022 Jun 28;23(13):7180.
RGC neurons 200 µM 3 min Lamotrigine significantly reduced the firing rates in Nf1+/neoRGC neurons, indicating its role in modulating neuronal excitability through HCN channel activation. Nat Commun. 2022 May 19;13(1):2785.
NT2-N cells 50 μM 24 h To evaluate the transcriptomic effects of Lamotrigine in combination with other drugs on NT2-N cells, results showed that Lamotrigine had a synergistic effect in the drug cocktail, influencing the expression of ANXA2, FBN1, and TPP3 genes. Bipolar Disord. 2023 Dec;25(8):661-670.

Lamotrigine/拉莫三嗪 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice VTAVgat-CASP3 mice Intraperitoneal injection 10 mg/kg Single or repeated treatments Lamotrigine had no therapeutic effect on the mania-like behavior of VTAVgat-CASP3 mice, neither affecting their locomotor activity nor the immobility time during the tail suspension test. Mol Psychiatry. 2021 Sep;26(9):5213-5228
Mice Nf1-OPG model Intraperitoneal injection 25 mg/kg Three times a week for 6 weeks Lamotrigine treatment reduced OPG development, decreased optic nerve proliferation, microglia, and T-cell content, indicating that HCN channel activation can block OPG progression. Nat Commun. 2022 May 19;13(1):2785.
Mice Non-alcoholic steatohepatitis (NASH) model Intravenous injection 10.2 ng/mL Single dose Lamotrigine was used as an internal standard for UPLC-MS/MS analysis and was not directly used for the treatment of NASH. J Adv Res. 2022 Jul;39:319-332
Mice Wild-type and FHM1 mutant mice Oral gavage 30 mg/kg Once daily for 7 weeks Chronic lamotrigine treatment reduces the susceptibility to KCl- or electrical stimulation-induced spreading depressions as well as ischemic depolarizations in both wild-type and familial hemiplegic migraine type 1 mutant mice, consequently improving tissue and neurological outcomes. A single dose of the drug is ineffective. Stroke. 2015 Jan;46(1):229-36
Mice Nf1f/neo; hGFAP-Cre (Nf1-OPG) mouse model Intraperitoneal injection 25 mg/kg Three times a week for 6 weeks Lamotrigine treatment reduced tumor progression in Nf1-OPG mice, decreasing optic nerve proliferation, microglia, and T-cell content, indicating that HCN channel activation can inhibit tumor progression. Nat Commun. 2022 May 19;13(1):2785.

Lamotrigine/拉莫三嗪 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00206778 Mixed Mania Bipolar Disorder Phase 2 Completed - United States, New York ... 展开 >> Beth Israel Medical Center New York, New York, United States, 10003 收起 <<
NCT00104416 Epilepsy, Tonic-Clonic Phase 3 Completed - -
NCT02283801 Epilepsy Phase 1 Completed - -

Lamotrigine/拉莫三嗪 参考文献

[1]Goa KL, Ross SR, et al. Lamotrigine. A review of its pharmacological properties and clinical efficacy in epilepsy. Drugs. 1993 Jul;46(1):152-76.

[2]Leach MJ, Marden CM, et al. Pharmacological studies on lamotrigine, a novel potential antiepileptic drug: II. Neurochemical studies on the mechanism of action. Epilepsia. 1986 Sep-Oct;27(5):490-7.

[3] Lovrić M, Čajić I, Petelin Gadže Ž, Klarica Domjanović I, Božina N. Effect of antiepileptic drug comedication on lamotrigine concentrations. Croat Med J. 2018 Feb 28;59(1):13-19.

[4]Kim KJ, Jeun SH, Sung KW. Lamotrigine, an antiepileptic drug, inhibits 5-HT3 receptor currents in NCB-20 neuroblastoma cells. Korean J Physiol Pharmacol. 2017 Mar;21(2):169-177.

[5]Jun IG, Kim SH, Yoon YI, Park JY. Intrathecal lamotrigine attenuates antinociceptive morphine tolerance and suppresses spinal glial cell activation in morphine-tolerant rats. J Korean Med Sci. 2013 Feb;28(2):300-7.

[6]Wang K, Fernandez-Escobar A, Han S, Zhu P, Wang JH, Sun Y. Lamotrigine Reduces Inflammatory Response and Ameliorates Executive Function Deterioration in an Alzheimer's-Like Mouse Model. Biomed Res Int. 2016;2016:7810196

Lamotrigine/拉莫三嗪 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.90mL

0.78mL

0.39mL

19.52mL

3.90mL

1.95mL

39.05mL

7.81mL

3.90mL

Lamotrigine/拉莫三嗪 技术信息

CAS号84057-84-1
分子式C9H7Cl2N5
分子量 256.09
SMILES Code NC1=NC(N)=C(C2=CC=CC(Cl)=C2Cl)N=N1
MDL No. MFCD00865333
别名 LTG; BW430C; Lamotrigine, Lamictal, BW-430C, Crisomet, Lamictin, Lamitor
运输蓝冰
InChI Key PYZRQGJRPPTADH-UHFFFAOYSA-N
Pubchem ID 3878
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 25 mg/mL(97.62 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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