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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| 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+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| 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. |
| 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. |
| 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 | - | - |
| 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 |
|
| 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 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
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