Flupirtine Maleate

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Chemical Structure| 75507-68-5 同义名 : 氟吡啶马来酸 ;Flupirtine (maleate)
CAS号 : 75507-68-5
货号 : A508491
分子式 : C19H21FN4O6
纯度 : 98%
分子量 : 420.39
MDL号 : MFCD00941415
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
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

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].
实验方案
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
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.