Home DNA Damage/DNA Repair DNA/RNA Synthesis antagonist - iGluR antagonist Flupirtine maleate

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Flupirtine maleate DNA/RNA Synthesis antagonist

Cat.No.S1334

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 DNA/RNA Synthesis antagonist Chemical Structure

Chemical Structure

Molecular Weight: 420.39

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Chemical Information, Storage & Stability

Molecular Weight 420.39 Formula

C15H17FN4O2·C4H4O4

 Storage (From the date of receipt)
CAS No. 75507-68-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCOC(=O)NC1=C(N=C(C=C1)NCC2=CC=C(C=C2)F)N.C(=CC(=O)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (199.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
NMDA receptor [1]
Potassium channel [6]
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]
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]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10988329/
  • [5] https://pubmed.ncbi.nlm.nih.gov/9134985/
  • [6] https://pubmed.ncbi.nlm.nih.gov/10599868/
  • [7] https://pubmed.ncbi.nlm.nih.gov/9134985/
  • [8] https://pubmed.ncbi.nlm.nih.gov/9554586/
  • [9] https://pubmed.ncbi.nlm.nih.gov/11472262/

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