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Flupirtine maleate(D 9998)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Flupirtine maleate(D 9998)图片
CAS NO:75507-68-5
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)420.39
FormulaC15H17FN4O2·C4H4O4
CAS No.75507-68-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 84 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (4.8 mM)
Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
SynonymsW-2964M; W-2964; W2964M; W2964; W 2964M; W 2964; D-9998; Katadolon.
实验参考方法
In Vitro

In vitro activity: Flupirtine pre-incubated for 2 hours prevents cell death in rat cortical neurons induced by NMDA and gp120 of HIV-1. Flupirtine is capable of protecting primary neurons against glutamate-induced cytotoxicity by reducing calcium ion concentrations at 1-10 mM. Flupirtine pretreated for 2 hours preventsβ-amyloid-induced apoptosis in primary neuronal cells at concentrations of 1 or 5μg/mL.


Cell Assay: For measurement of viability and generation of reactive oxygen intermediates, PC12 cells are seeded in 24- or 96-well plates coated with poly-L-lysine at 105 cells/mL. Drugs are dissolved in PBS (pH 7.4), or ethanol and filtered sterile. At the end of each experiment cells are trypsinized and pelleted together with cells of the culture supernatant. After staining for 10 min with 0.2% Trypan blue solution live (unstained) and dead (Trypan blue positive) cells are counted in a hemocytometer chamber. In addition, cellular viability is evaluated by the reduction of MTT to formazan. After 2 hours incubation with MTT (0.5 mg/ml) at 37 °C, cells are lysed in DMSO. Extinction at 570 nm is determined on a plate photometer. For staining of surviving adherent cells, plates are incubated for 10 min with 0.5% crystalviolet dissolved in 20% methanol. Plates are rinsed with water and stained cells are lysed in 50% ethanol, 0.1 M sodiumcitrate before determining extinction at 550 nm.

In VivoPre-treatment with Flupirtine exerts a protective effect on hippocampal and striatal neuronal damage and on deficits in spatial learning in rats with cerebral ischemia. Flupirtine administered centrally inhibits the nociceptive responses induced by chemical, thermal, mechanical and electrical stimuli in animal studies. Flupirtine exerts muscle relaxant effects in rat.
Animal modelMale Wistar rats with cerebral ischemia induced by four-vessel-occlusion
Formulation & DosageFormulated in 0.9% sodium chloride solution; 5 mg/kg; i.p. injection
References

Eur J Pharmacol. 1994 Dec 15;288(1):27-33; Eur J Pharmacol. 1995 Dec 29;294(2-3):469-73; Brain Res. 1997 Apr 18;754(1-2):279-84.