| Bioactivity | Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research[1][2][3][4][5]. |
| Target | IC50: 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block (sodium channel of HEK293 transfected with hNav1.5 plasmid) |
| Invitro | Mexiletine (10µM, 48 h) 在转染 SCN5A-WT 或 SCN5A-1795insD 的 HEK293A 细胞中增加了峰值 INa 和晚期 INa，Mexiletine (10µM, 5 min) 阻断了晚期 INa[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Mexiletine 相关抗体: |
| In Vivo | Mexiletine (30, 100 mg/kg, 口服, 急性给药) 逆转 Oxaliplatin (HY-17371) 诱导的大鼠机械痛觉过敏和低温痛觉过敏[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 31828-71-4 |
| Formula | C11H17NO |
| Molar Mass | 179.26 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Campbell RW, et al. Mexiletine. N Engl J Med. 1987，316(1):29-34. [2]. De Bellis M, et al. Combined modifications of mexiletine pharmacophores for new lead blockers of Na(v)1.4 channels. Biophys J. 2013，104(2):344-54. [3]. Nasilli G, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010;112(4):473-6. [4]. Egashira N, et al. Mexiletine reverses oxaliplatin-induced neuropathic pain in rats. J Pharmacol Sci. 2010，112(4):473-6. |