2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Potassium Channel iGluR GABA Receptor
  4. Flupirtine Maleate

Flupirtine Maleate  (Synonyms: D 9998 Maleate)

Cat. No.: HY-17001 Purity: 99.97%
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Flupirtine (D 9998) Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

For research use only. We do not sell to patients.

Flupirtine Maleate

Flupirtine Maleate Chemical Structure

CAS No. : 75507-68-5

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Based on 1 publication(s) in Google Scholar

Other Forms of Flupirtine Maleate:

Flupirtine Maleate Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Flupirtine Maleate

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  • Biological Activity

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  • References

  • Customer Review

Description

Flupirtine (D 9998) Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis[1][2][3][4][5].

IC50 & Target

NMDA Receptor

 

In Vitro

Flupirtine (0.1-100 μM for tsA cells; 3-30 μM for SCG neurons; 3-30 μM for hippocampal, DRG, DH neurons) Maleate enhances currents through KV7 channels in tsA 201 cells expressing KV7.2/7.3 subunits, rat SCG neurons, hippocampal neurons, DRG neurons, and DH neurons with EC50 values ranging from 4.4 to 6.1 μM[2].
Flupirtine (10, 30 μM) Maleate modulates GABAA receptors (enhancing low-concentration GABA currents) and NMDA receptors (inhibiting at 30 μM) but not TRPV1, non-NMDA glutamate, or glycine receptors in rat hippocampal neurons[2].
Flupirtine (30 μM) Maleate potentiates GABAA receptors in rat DRG, DH, and SCG neurons, with greater leftward shifts of GABA concentration-response curves in DRG and DH neurons than SCG neurons[2].
Flupirtine (0.1-100 μM) Maleate is more potent at enhancing GABAA receptor currents in rat DRG neurons (EC50 22 μM) than DH (EC50 53 μM) or hippocampal (EC50 65 μM) neurons, and therapeutic concentrations (3 μM) facilitate KV7 channels and GABAA receptors similarly in DRG/DH neurons[2].
Flupirtine (10-300 μM; 1.5 minutes) Maleate antagonizes NMDA-induced currents in cultured rat superior colliculus neurones with an IC50 of 182.1 μM for steady-state responses and 228.6 μM for peak responses[3].
Flupirtine (0.001-10 mM; 24 h) Maleate inhibits the growth of U373 MG cells with a GI50 of 0.47 mM, showing significant growth reduction at 1 and 10 mM after 24 h[4].
Flupirtine (1 mM; 24, 48 h) Maleate alters the cell cycle distribution of U373 MG cells, decreasing the percentage of cells in the G0-G1 phase compared to control after 24 and 48 h, with significant variations in cell cycle phases observed after 48 h[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Flupirtine Maleate Related Antibodies

Cell Viability Assay[4]

Cell Line: U373 malignant glioma cell lines
Concentration: 0.001, 0.01, 0.1, 1, and 10 mM
Incubation Time: 24 hours
Result: Inhibited U373 MG cell growth with a GI50 of 0.47. Significantly reduced cell growth at high doses (1 and 10 mM) compared to low doses (0.001 to 0.1 mM) and control.

Cell Cycle Analysis[4]

Cell Line: U373 malignant glioma cell lines
Concentration: 1 mM
Incubation Time: 24 h; 48 h
Result: Detected G0-G0 phase percentage of 45.48, Sub G0-G0 phase percentage of 2.49, S phase percentage of 24.47, and G₂-M phase percentage of 27.56 after 24 h treatment. Detected G0-G1 phase percentage of 56.39, Sub G0-G1 phase percentage of 1.82, S phase percentage of 18.99, and G2-M phase percentage of 22.80 after 48 h treatment. Observed significant variations in cell cycle phases after 48 h but not 24 h of treatment.
In Vivo

Flupirtine (1-10 mg/kg; i.p.; single dose; up to 9 h post-stroke) Maleate induces sustained neuroprotection, enhanced neurological recovery, and angioneurogenesis in mice with transient focal cerebral ischemia, with 10 mg/kg being the most effective dose[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL6 (male, 22-25 g, transient focal cerebral ischemia via left middle cerebral artery thread occlusion for 30 min)[1]
Dosage: 1, 5, 10 mg/kg; 10 mg/kg (majority of experiments)
Administration: i.p.; single dose; during reperfusion or at 3, 6, 9, 12 h post-stroke (9 h post-stroke for majority of experiments)
Result: Reduced infarct volumes on day 2 post-stroke at 5 and 10 mg/kg (1 mg/kg had no effect); reduced infarct volumes, TUNEL+ cell counts, rt-PA-induced acute brain toxicity, Evans blue extravasation, oxidative stress (TBARS formation), intracerebral leukocyte infiltration, calpain activity, JNK and NF-κB activation, and proteasomal activity at 10 mg/kg (given up to 9 h post-stroke); increased STAT6 abundance, neuronal density (NeuN+ cells), CD31+ endothelial cells, Dcx+ immature neurons, and BrdU+/NeuN+ mature neurons on day 84; improved performance in rota rod, tight rope, corner turn, and foot fault tests up to day 84 at 10 mg/kg (given up to 9 h post-stroke).
Clinical Trial
Molecular Weight

420.39

Formula

C19H21FN4O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(N=C1N)NCC2=CC=C(C=C2)F)OCC.O=C(/C=C\C(O)=O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (237.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 1.43 mg/mL (3.40 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.97%

SDS (393 KB)

COA (245 KB) HNMR (148 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.3787 mL 11.8937 mL 23.7874 mL 59.4686 mL
DMSO 5 mM 0.4757 mL 2.3787 mL 4.7575 mL 11.8937 mL
10 mM 0.2379 mL 1.1894 mL 2.3787 mL 5.9469 mL
15 mM 0.1586 mL 0.7929 mL 1.5858 mL 3.9646 mL
20 mM 0.1189 mL 0.5947 mL 1.1894 mL 2.9734 mL
25 mM 0.0951 mL 0.4757 mL 0.9515 mL 2.3787 mL
30 mM 0.0793 mL 0.3965 mL 0.7929 mL 1.9823 mL
40 mM 0.0595 mL 0.2973 mL 0.5947 mL 1.4867 mL
50 mM 0.0476 mL 0.2379 mL 0.4757 mL 1.1894 mL
60 mM 0.0396 mL 0.1982 mL 0.3965 mL 0.9911 mL
80 mM 0.0297 mL 0.1487 mL 0.2973 mL 0.7434 mL
100 mM 0.0238 mL 0.1189 mL 0.2379 mL 0.5947 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Flupirtine Maleate Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Flupirtine75507-68-5D 9998D9998D-9998Potassium ChanneliGluRGABA ReceptorKcsAIonotropic glutamate receptorsGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorbrainpenetrantnon-opioidcentrallyactinganalgesicNMDARNeuroprotectivestrokeInhibitorinhibitorinhibit

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