Flupirtine maleate

SKU: orb1300710

Description

Flupirtine maleate (Katadolon maleate) is the salt form of Flupirtine, a centrally acting, non-opioid analgesic. It functions as an NMDA receptor antagonist and a selective neuronal potassium channel opener. This compound is utilized in research areas such as neuropharmacology and pain mechanisms, applicable in both in vitro receptor studies and in vivo animal models of analgesia.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 75507-68-5
• MW: 420.39
• Purity: 99.50%
• Formula: C₁₅H₁₇FN₄O₂·C₄H₄O₄
• SMILES: CCOC(=O)Nc1c(nc(cc1)NCc1ccc(cc1)F)N.C(=C\C(=O)O)\C(=O)O
• Target: iGluR,Potassium Channel,NMDAR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.76 mM);DMSO:50 mg/mL (118.94 mM);Ethanol:4.21 mg/mL (10.01 mM)

Bioactivity

• In Vivo:
  Flupirtine was able to block NMDA and gp120 HIV-1-induced cell death in rat cortical neurons.Flupirtine at concentrations of 1 μM and 10 μM reduced TRAIL-regulated death of human living brain tissue in culture; a concentration of 10 μM in 10 mM L-glutamic acid-treated PC 12 cultures significantly reduced non-receptor- regulated necrotic cell death; a concentration of 1 or 5 μg/mL blocked β-amyloid (25-35)-induced apoptosis by acting on primary neuronal cells; and a concentration of 1-10 mM protected primary neuronal cells from monosodium glutamate-induced toxicity by lowering calcium ion concentration.
• In Vitro:
  Flupirtine was able to block NMDA and gp120 HIV-1-induced cell death in rat cortical neurons.Flupirtine at concentrations of 1 μM and 10 μM reduced TRAIL-regulated death of human living brain tissue in culture; a concentration of 10 μM in 10 mM L-glutamic acid-treated PC 12 cultures significantly reduced non-receptor- regulated necrotic cell death; a concentration of 1 or 5 μg/mL blocked β-amyloid (25-35)-induced apoptosis by acting on primary neuronal cells; and a concentration of 1-10 mM protected primary neuronal cells from monosodium glutamate-induced toxicity by lowering calcium ion concentration.
• Cell Research:
  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. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Flupirtine, Flupirtine maleate, Flupirtine Maleate, Inhibitor, iGluR, Ionotropic glutamate receptors, non-opioid, KcsA, inhibit, Katadolon Maleate, Katadolon maleate, Neuroprotective, NMDA receptor, NMDAR, acting, brain,?penetrant, analgesic, centrally, stroke, Potassium Channel, PotassiumChannel

Compound Identifiers

PubChem CID

6435335