货号:A200751 同义名: KOE-1173 hydrochloride;Mexiletine (hydrochloride)
Mexiletine HCl is a non-selective blocker of voltage-gated sodium channel. It blongs to the anti-arrhythmic compounds of class IB .
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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% | |||||||||||||||||
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。 |
靶点 |
|
描述 | Mexiletine is an orally effective antiarrhythmic agent noted for its benefits in treating myotonia and neuropathic pain. It operates by inhibiting sodium channels, with an IC50 of 75±8 μM for tonic block and 23.6±2.8 μM for use-dependent block, making it relevant for both cardiovascular and neurological research[1].[2].[3].[4].[5]. |
体内研究 | Additionally, Mexiletine (30, 100 mg/kg, p.o., acutely administered) effectively counteracts mechanical allodynia and cold hyperalgesia in rats induced with Oxaliplatin[4]. |
体外研究 | Mexiletine (10µM, 48 h) enhances both peak INa and late INa in HEK293A cells transfected with SCN5A-WT or SCN5A-1795insD, while a shorter exposure (10µM, 5 min) inhibits the late INa[3]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02308748 | Drug-induced QT Prolongation ... 展开 >> Pharmacokinetics Pharmacodynamics 收起 << | Phase 1 | Completed | - | - |
NCT02336477 | Non-dystrophic Myotonias ... 展开 >> Paramyotonia Congenita Myotonia Congenita 收起 << | Phase 3 | Completed | - | France ... 展开 >> Groupe Hospitalier Pitié Salpetriere Paris, France, 75013 收起 << |
NCT02045667 | Non Dystrophic Myotonia | Phase 2 | Completed | - | Netherlands ... 展开 >> Departments of Neurology, Radboud University Nijmegen Medical Centre, the Netherlands Nijmegen, Gelderland, Netherlands, 6500HB 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.64mL 0.93mL 0.46mL |
23.18mL 4.64mL 2.32mL |
46.36mL 9.27mL 4.64mL |
CAS号 | 5370-01-4 |
分子式 | C11H18ClNO |
分子量 | 215.72 |
别名 | KOE-1173 hydrochloride;Mexiletine (hydrochloride);Ko 1173;Mexiletine hydrochloride |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 40 mg/mL(185.43 mM),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 H2O: 100 mg/mL(463.56 mM),配合低频超声助溶 |
动物实验配方 |