产品
编 号：F572463
分子式：C11H18ClNO
分子量：215.72
分子式：C11H18ClNO
分子量：215.72
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
100mg
400
In-stock
500mg
560
In-stock
结构图
CAS No: 5370-01-4
产品详情
生物活性：
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.
体内研究：
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。Animal Model:Male Sprague-Dawley rats with Oxaliplatin (HY-17371)-induced neuropathic pain
Dosage:Oxaliplatin (4 mg /kg) and Mexiletine(10, 30, 100 mg/kg)
Administration:Oxaliplatin, Intraperitoneal injection (i.p.)in days 1, 2, 8, 9, 15, 16, 22, and 23; Mexiletine, Oral gavage (p.o.), acute administration
Result:100 mg/kg completely reversed the reduction of 50% paw withdrawal threshold by Oxaliplatin at 60 min after administration in the von Frey test, completely reversed the increase of number of withdrawal responses at 60 and 120 min after administration in the acetone test. 30 mg/kg partly reversed the symptom and 10 mg/kg did not reverse any symptom. The effect disappeared by 180 min after administration.
体外研究：
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。
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.
体内研究：
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。Animal Model:Male Sprague-Dawley rats with Oxaliplatin (HY-17371)-induced neuropathic pain
Dosage:Oxaliplatin (4 mg /kg) and Mexiletine(10, 30, 100 mg/kg)
Administration:Oxaliplatin, Intraperitoneal injection (i.p.)in days 1, 2, 8, 9, 15, 16, 22, and 23; Mexiletine, Oral gavage (p.o.), acute administration
Result:100 mg/kg completely reversed the reduction of 50% paw withdrawal threshold by Oxaliplatin at 60 min after administration in the von Frey test, completely reversed the increase of number of withdrawal responses at 60 and 120 min after administration in the acetone test. 30 mg/kg partly reversed the symptom and 10 mg/kg did not reverse any symptom. The effect disappeared by 180 min after administration.
体外研究：
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。
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