Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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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. In the past, flupirtine was used as an analgesic for both acute and persistent pain.
Targets |
Potassium channel; NMDA receptor
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ln Vitro |
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ln Vivo |
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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.
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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 |
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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. |
Molecular Formula |
C19H21FN4O6
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Molecular Weight |
420.39
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Exact Mass |
304.13
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Elemental Analysis |
C, 54.28; H, 5.04; F, 4.52; N, 13.33; O, 22.83
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CAS # |
75507-68-5
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Related CAS # |
56995-20-1; 33400-45-2 (HCl); 75507-68-5; 815586-85-7 (gluconate)
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Appearance |
Solid powder
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SMILES |
CCOC(=O)NC1=C(N=C(C=C1)NCC2=CC=C(C=C2)F)N.C(=C\C(=O)O)\C(=O)O
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InChi Key |
DPYIXBFZUMCMJM-BTJKTKAUSA-N
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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-
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Chemical Name |
(Z)-but-2-enedioic acid;ethyl N-[2-amino-6-[(4-fluorophenyl)methylamino]pyridin-3-yl]carbamate
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.95 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% Propylene glycol , 5% Tween 80 , 65% D5W: 30 mg/mL |
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.
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.
(2) Be sure to add the solvent(s) in order.