Lamotrigine N2-oxide
(Synonyms: 拉莫三嗪N2-氧化物) 目录号 : GC49538
A metabolite of lamotrigine
Cas No.:136565-76-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Lamotrigine N2-oxide is a metabolite of the voltage-gated sodium channel inhibitor lamotrigine .1
1.Doig, M.V., and Clare, R.A.Use of thermospray liquid chromatography-mass spectrometry to aid in the identification of urinary metabolites of a novel antiepileptic drug, LamotrigineJ. Chromatogr.554(1-2)181-189(1991)
| Cas No. | 136565-76-9 | SDF | Download SDF |
| 别名 | 拉莫三嗪N2-氧化物 | ||
| Canonical SMILES | NC(N=C(N)C(C1=CC=CC(Cl)=C1Cl)=N2)=[N]2=O | ||
| 分子式 | C9H7Cl2N5O | 分子量 | 272.1 |
| 溶解度 | DMSO: slightly,Methanol: slightly | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6751 mL | 18.3756 mL | 36.7512 mL |
| 5 mM | 0.735 mL | 3.6751 mL | 7.3502 mL |
| 10 mM | 0.3675 mL | 1.8376 mL | 3.6751 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Simultaneous determination of plasma lamotrigine, lamotrigine N2-glucuronide and Lamotrigine N2-oxide by UHPLC-MS/MS in epileptic patients
J Pharm Biomed Anal 2022 Oct 25;220:115017.PMID:36030754DOI:10.1016/j.jpba.2022.115017.
The plasma concentration of lamotrigine (LTG) and its metabolites has great interindividual variability. An UHPLC-MS/MS method for simultaneous determination of LTG and lamotrigine N2-glucuronide (LTG N2-GLUC), Lamotrigine N2-oxide was developed, validated, and applied in 58 plasma samples. The ion transition was m/z 256.0 > 144.9 for LTG, 432.1 > 256.0 for LTG N2-GLUC, 272.2 > 241.9 for LTG N2-oxide, and 259.1 > 144.8 for LTG-13C3 (internal standard). The flow rate was 0.4 mL/min with a run time of 3 min. The calibration range was 0.025-2 mg/L for LTG and LTG N2-GLUC, and 0.000625-0.05 mg/L for LTG N2-oxide. For all analytes, the intra-day and inter-day bias and imprecision were -11.7-5.7 % and less than 14.3 %, and the internal standard normalized recovery and matrix factor were 91.7-101.5 % and 98.1-110.1 % with CV < 13. 7%. Ten- and twenty-fold dilution with blank plasma did not affect the analysis. All analytes were stable in plasma at room temperature for 8 h, at -80 °C for 80 days, and after 3 freeze-thaw cycles. The LTG N2-GLUC/LTG ratio was 0.44 in LTG monotherapy group. The ratio was reduced to 0.17 when co-administrated with valproic acid, while elevated to 0.82 when co-administrated with enzyme inducer. In conclusion, this method is suitable for simultaneous determination of LTG, LTG N2-GLUC and LTG N2-oxide in human plasma.
UDP-glucuronosyltransferase 1A4-mediated N2-glucuronidation is the major metabolic pathway of lamotrigine in chimeric NOG-TKm30 mice with humanised-livers
Xenobiotica 2021 Oct;51(10):1146-1154.PMID:34423713DOI:10.1080/00498254.2021.1972492.
Lamotrigine is a phenyltriazine anticonvulsant used to treat epilepsy and bipolar disorder, with species-dependent metabolic profiles. In this study, we investigated the metabolism of lamotrigine in chimeric NOG-TKm30 mice transplanted with human hepatocytes (humanised-liver mice).Substantial lamotrigine N2-glucuronidation activities were observed in the liver microsomes from humanised-liver mice, humans, marmosets, and rabbits, compared to those from monkeys, minipigs, guinea pigs, rats, and mice. Lamotrigine N2-glucuronidation activities in the liver microsomes from humanised-liver mice were dose-dependently inhibited by hecogenin, a specific inhibitor of the human UGT1A4.The major metabolite in the hepatocytes from humanised-liver mice and humans was lamotrigine N2-glucuronide, whereas that in mouse hepatocytes was Lamotrigine N2-oxide. After a single oral dose of lamotrigine (10 mg/kg), the plasma levels of N2-glucuronide, N5-glucuronide, and N2-methyl were higher in humanised-liver mice compared to that in NOG-TKm30 mice. Lamotrigine N2-glucuronide was the most abundant metabolite in the urine in humanised-liver mice, similar to that reported in humans; whereas, Lamotrigine N2-oxide was predominantly excreted in the urine in NOG-TKm30 mouse.These results suggest that humanised-liver mice may be a suitable animal model for studying the UGT1A4 mediated-lamotrigine metabolism.