Home DNA Damage/DNA Repair DNA/RNA Synthesis antagonist Flupirtine maleate For research use only.

Flupirtine maleate

Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.

Flupirtine maleate Chemical Structure

Flupirtine maleate Chemical Structure

CAS: 75507-68-5

Selleck's Flupirtine maleate has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Biological Activity

Description Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.
Targets
NMDA receptor [1] Potassium channel [6]
In vitro
In vitro Flupirtine pre-incubated for 2 hours prevents cell death in rat cortical neurons induced by NMDA and gp120 of HIV-1. [1] Flupirtine is capable of protecting primary neurons against glutamate-induced cytotoxicity by reducing calcium ion concentrations at 1-10 mM. [2] Flupirtine pretreated for 2 hours preventsβ-amyloid-induced apoptosis in primary neuronal cells at concentrations of 1 or 5μg/mL. [3] Flupirtine at concentration of 10 μM markedly decreases nonreceptor-mediated necrotic cell death in PC 12 cultures treated with 10 mM L-glutamate, meanwhile, Flupirtine exerts anti-oxidative effects in PC 12 cultures. [4] Flupirtine-maleate at concentrations of 1 μM and 10 μM decreases TRAIL-mediated death of human living brain tissue culture. [5] Flupirtine activates inwardly rectifying potassium ion channels and thus stabilizes the resting membrane potential at a therapeutically relevant concentration. [6]
Cell Research Cell lines PC12 cell
Concentrations 1 or 5 μg/mL
Incubation Time 72 hours
Method

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 Vivo
In vivo Pre-treatment with Flupirtine exerts a protective effect on hippocampal and striatal neuronal damage and on deficits in spatial learning in rats with cerebral ischemia. [7] Flupirtine administered centrally inhibits the nociceptive responses induced by chemical, thermal, mechanical and electrical stimuli in animal studies. [8] Flupirtine exerts muscle relaxant effects in rat. [9]
Animal Research Animal Models male Wistar rats with cerebral ischemia induced by four-vessel-occlusion
Dosages 5 mg/kg
Administration Intraperitoneal injection either 20 min before and 50 min after occlusion or directly and 70 min after occlusion

Chemical lnformation & Solubility

Molecular Weight 420.39 Formula

C15H17FN4O2·C4H4O4
CAS No. 75507-68-5 SDF Download Flupirtine maleate SDF
Smiles CCOC(=O)NC1=C(N=C(C=C1)NCC2=CC=C(C=C2)F)N.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (199.81 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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