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

货号:A551325 同义名: LTG;BW430C

Lamotrigine is a member of the sodium channel blocking class of antiepileptic drugs which can block L-, N-, and P-type calcium channels and has weak 5-HT3 receptor inhibition.

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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 化学结构 CAS号:84057-84-1
Lamotrigine 化学结构
CAS号:84057-84-1
Lamotrigine 3D分子结构
CAS号:84057-84-1
Lamotrigine 化学结构 CAS号:84057-84-1
Lamotrigine 3D分子结构 CAS号:84057-84-1
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Lamotrigine 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 95%
Zegocractin ++

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

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

hCaV3.2, IC50: 110 nM

hCaV3.1, IC50: 50 nM

99%+
Dronedarone Hydrochloride 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

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

NCX, IC50: 33 nM

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

Calcium channel, Ki: 68 nM

95%
Lomerizine 2HCl 98%
Efonidipine 98%
Levamlodipine 97%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

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

Calcium channel, IC50: 2.6 nM

98%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

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

Calcium channel, IC50: 0.03 nM

98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

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

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

97%
Cilnidipine 98%
Cinepazide Maleate 98%
Terfenadine 98%
YM-58483 99%+
Ranolazine 98%
Praeruptorin A p38 MAPK,Akt 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%
Lamotrigine 98%
Vinpocetine 98%
Zonisamide 98%
Dronedarone Hydrochloride 95%
Procainamide hydrochloride 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%
Ambroxol 98+%
Primidone 99%
Propafenone 99%
A-803467 ++++

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

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

Voltage-gated sodium channel, ED50: 3.4 mM

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 生物活性

靶点
  • 5-HT

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

    5-HT (rat brain synaptosomes), IC50:474 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 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 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 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 技术信息

CAS号84057-84-1
分子式C9H7Cl2N5
分子量 256.091
别名 LTG;BW430C;Lamotrigine, Lamictal, BW-430C, Crisomet, Lamictin, Lamitor
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

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

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