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马来酸氟吡汀 /Flupirtine Maleate {[allProObj[0].p_purity_real_show]}

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。

Flupirtine Maleate 化学结构 CAS号:75507-68-5
Flupirtine Maleate 化学结构
CAS号:75507-68-5
Flupirtine Maleate 3D分子结构
CAS号:75507-68-5
Flupirtine Maleate 化学结构 CAS号:75507-68-5
Flupirtine Maleate 3D分子结构 CAS号:75507-68-5
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Flupirtine Maleate 纯度/质量文件 产品仅供科研

货号:A508491 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Flupirtine Maleate 生物活性

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].

Flupirtine Maleate 参考文献

[1]Jan Dörr,et al. Disease Modification in Multiple Sclerosis by Flupirtine-Results of a Randomized Placebo Controlled Phase II Trial. Front Neurol. 2018 Oct 9;9:842.

[2]Hanna M Jaeger, et al. The indirect NMDAR inhibitor flupirtine induces sustained post-ischemic recovery, neuroprotection and angioneurogenesis. Oncotarget. 2015 Jun 10;6(16):14033-44.

[3]Elango Panchanathan,Effect of flupirtine on the growth and viability of U373 malignant glioma cells.Cancer Biol Med. 2013 Sep;10(3):142-7.

[4]Martin J Gunthorpe,et al. The mechanism of action of retigabine (ezogabine), a first-in-class K+ channel opener for the treatment of epilepsy.Epilepsia. 2012 Mar;53(3):412-24.

Flupirtine Maleate 实验方案

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

Flupirtine Maleate 技术信息

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

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