Flupirtine maleate (D 9998)

Alias: W-2964M; W-2964; W2964M; W2964;W 2964M; W 2964; D-9998; Katadolon
Cat No.:V1475 Purity: ≥98%
Flupirtine maleate(W2964; W-2964M; D9998;W-2964; D-9998; Katadolon), the maleate salt form of Flupirtine, is a centrally acting non-opioid analgesic agent and a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.
Flupirtine maleate (D 9998) Chemical Structure CAS No.: 75507-68-5
Product category: DNA(RNA) Synthesis
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Flupirtine maleate (W2964; W-2964M; D9998; W-2964; D-9998; Katadolon), the maleate salt form of Flupirtine, is a centrally acting non-opioid analgesic agent and a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. In the past, flupirtine was used as an analgesic for both acute and persistent pain.

Biological Activity I Assay Protocols (From Reference)
Targets
Potassium channel; NMDA receptor
ln Vitro

Flupirtine Pre-incubated for two hours inhibits the NMDA- and HIV-1-gp120-induced cell death in rat cortical neurons.[1] Flupirtine lowers calcium ion concentrations at 1–10 mM, shielding primary neurons from glutamate-induced cytotoxicity. At concentrations of 1 or 5μg/mL, β-amyloid-induced apoptosis in primary neuronal cells is inhibited by a 2-hour pretreatment with flupirtine.[3] When PC 12 cultures are treated with 10 mM L-glutamate, flupirtine at a concentration of 10 μM significantly reduces nonreceptor-mediated necrotic cell death. Flupirtine also has anti-oxidative effects on PC 12 cultures.[4] Flupirtine-maleate at 1 μM and 10 μM concentrations reduces the death of human living brain tissue culture mediated by TRAIL.[5] The resting membrane potential is stabilized at a therapeutically relevant concentration by flupirtine through the activation of inwardly rectifying potassium ion channels.[6]

ln Vivo
pretreatment with flupirtine prevents damage to the hippocampus and striatum as well as deficits in spatial learning in rats with cerebral ischemia. Animal studies have shown that the administration of flupirtine centrally inhibits nociceptive responses induced by chemical, thermal, mechanical, and electrical stimuli.[8] Flupirtine has a calming effect on the muscles of rats.[9]
Cell Assay
In order to assess the generation of reactive oxygen intermediates and viability, PC12 cells are plated at a density of 105 cells/mL in 24- or 96-well plates coated with poly-L-lysine. The drugs are dissolved in ethanol or PBS (pH 7.4) and then sterile filtered. Each experiment ends with the cells being trypsinized and pelleted along with the cells from the culture supernatant. In a hemocytometer chamber, live (unstained) and dead (Trypan blue positive) cells are counted following a 10-minute staining process with 0.2% Trypan blue solution. Furthermore, formazan is formed from the reduction of MTT to assess cellular viability. Cells are lysed in DMSO after being incubated with MTT (0.5 mg/ml) for two hours at 37°C. On a plate photometer, extinction at 570 nm is measured. Plates containing 0.5% crystalviolet dissolved in 20% methanol are incubated for 10 minutes in order to stain the adherent cells that remain viable. Before determining extinction at 550 nm, stained cells are lysed in 50% ethanol and 0.1 M sodium citrate on plates that have been rinsed with water.
Animal Protocol
male Wistar rats with cerebral ischemia induced by four-vessel-occlusion
5 mg/kg
Intraperitoneal injection either 20 min before and 50 min after occlusion or directly and 70 min after occlusion
References

[1]. Eur J Pharmacol . 1994 Dec 15;288(1):27-33.

[2]. Eur J Pharmacol . 1995 Dec 29;294(2-3):469-73.

[3]. J Neurochem . 1997 Jun;68(6):2371-7.

[4]. J Neural Transm (Vienna) . 1999;106(9-10):857-67.

[5]. J Neurochem . 1997 Jun;68(6):2371-7.

[6]. J Neural Transm, 1999, 106(9-10), 857-867.

[7]. Brain Res . 1997 Apr 18;754(1-2):279-84.

[8]. Cancer Chemother Pharmacol . 1998;41(6):437-47.

[9]. Curr Pharm Des . 2001 Sep;7(13):1199-212

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H21FN4O6
Molecular Weight
420.39
Exact Mass
304.13
Elemental Analysis
C, 54.28; H, 5.04; F, 4.52; N, 13.33; O, 22.83
CAS #
75507-68-5
Appearance
Solid powder
SMILES
CCOC(=O)NC1=C(N=C(C=C1)NCC2=CC=C(C=C2)F)N.C(=C\C(=O)O)\C(=O)O
InChi Key
DPYIXBFZUMCMJM-BTJKTKAUSA-N
InChi Code
InChI=1S/C15H17FN4O2.C4H4O4/c1-2-22-15(21)19-12-7-8-13(20-14(12)17)18-9-10-3-5-11(16)6-4-10;5-3(6)1-2-4(7)8/h3-8H,2,9H2,1H3,(H,19,21)(H3,17,18,20);1-2H,(H,5,6)(H,7,8)/b;2-1-
Chemical Name
(Z)-but-2-enedioic acid;ethyl N-[2-amino-6-[(4-fluorophenyl)methylamino]pyridin-3-yl]carbamate
Synonyms
W-2964M; W-2964; W2964M; W2964;W 2964M; W 2964; D-9998; Katadolon
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 84~100 mg/mL (~199.8~237.9 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
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3787 mL 11.8937 mL 23.7874 mL
5 mM 0.4757 mL 2.3787 mL 4.7575 mL
10 mM 0.2379 mL 1.1894 mL 2.3787 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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