货号:A508491 同义名: 氟吡啶马来酸 / Flupirtine (maleate)
Flupirtine Maleate是一种非阿片类的镇痛药,通过作用于 KV7 钾通道发挥作用,具有肌肉松弛和神经保护特性,同时间接拮抗 NMDA 受体和 GABAa 受体。
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产品名称 | Potassium Channel ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tolbutamide | ✔ | 98% | |||||||||||||||||
Glimepiride |
++++
SUR2B, IC50: 7.3 nM SUR1, IC50: 5.4 nM |
97% | |||||||||||||||||
Dronedarone Hydrochloride | ✔ | 95% | |||||||||||||||||
Gliquidone |
++
Potassium channel, IC50: 27.2 nM |
99% | |||||||||||||||||
TRAM-34 |
+++
IKCa1 (KCa3.1), Kd: 20 nM |
98% | |||||||||||||||||
Glibenclamide | ✔ | 98% | |||||||||||||||||
Amiodarone HCl | ✔ | 97% | |||||||||||||||||
Gliclazide |
++
Potassium channel, IC50: 184 nM |
98% | |||||||||||||||||
Repaglinide | ✔ | 98% | |||||||||||||||||
Dofetilide | ✔ | 98% | |||||||||||||||||
Nateglinide | ✔ | 99% | |||||||||||||||||
Quinine hydrochloride dihydrate | ✔ | 98% | |||||||||||||||||
ML133 HCl |
+
Kir2.1, IC50: 290 nM |
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。 |
描述 | Flupirtine maleate is a non-opioid central analgesic with strong permeability and high oral bioavailability. Flupirtine maleate is an indirect antagonist of N-methyl-D-aspartate receptor (NMDAR) with neuroprotective properties [1],[2]. |
体内研究 | Dosages of 5 and 10 mg/kg of Flupirtine have been shown to provide acute neuroprotection, alleviate motor coordination issues, and reduce toxicity caused by recombinant tissue plasminogen activator (rtPA)[2]. |
体外研究 | It functions indirectly as an antagonist to the N-methyl-D-aspartate receptor (NMDAR) and is known for its neuroprotective qualities. When administered to U373 malignant glioma cells at concentrations of 0.1, 1, and 10 mM over 24 hours, Flupirtine significantly inhibits cell growth and viability, with a GI50 of 0.47 mM, demonstrating its neuroprotective effects on these cells[3]. Furthermore, it interacts with KCNQ and GABAA channels within the 10-30 μM range[4]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.38mL 0.48mL 0.24mL |
11.89mL 2.38mL 1.19mL |
23.79mL 4.76mL 2.38mL |
CAS号 | 75507-68-5 |
分子式 | C19H21FN4O6 |
分子量 | 420.39 |
别名 | 氟吡啶马来酸 ;Flupirtine (maleate) |
运输 | 蓝冰 |
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,Room temperature |
溶解度 |
DMSO: 105 mg/mL(249.77 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 H2O: 1 mg/mL(2.38 mM),配合低频超声,并水浴加热至45℃助溶 |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear PO 0.5% CMC-Na 40 mg/mL suspension |