Flufenamic acid Immunology & Inflammation related inhibitor

Cat.No.S4268

Flufenamic Acid is an anti-inflammatory agent, and also acts as an ion channel modulator.
Flufenamic acid Immunology & Inflammation related inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 281.23

Quality Control

Batch: S426801 DMSO]56 mg/mL]false]Ethanol]56 mg/mL]false]Water]Insoluble]false Purity: 99.9%
99.9

Chemical Information, Storage & Stability

Molecular Weight 281.23 Formula

C14H10F3NO2

Storage (From the date of receipt)
CAS No. 530-78-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C(C(=C1)C(=O)O)NC2=CC=CC(=C2)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (199.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 56 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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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.

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Mechanism of Action

In vitro
Flufenamic acid reversibly inhibits ICl(Ca) in Xenopus oocytes with IC50 of 28 mM, elicit in response to depolarizing voltage steps, in a dose-dependent manner, with no effect on the shape of the current-voltage curve. [1] This compound blocks Ca2(+)-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells with IC50 of 10 μM. [2] It binds with high affinity and negative cooperativity (pH 7.6) to wild-type (KD1=30 nM, KD2=255 nM), V30M (KD1=41 nM, KD2=320 nM) and L55P transthyretin (KD1=74 nM, KD2=682 nM), completely inhibiting amyloid fibril formation at a concentration of 10.8 μM, 3× the physiological concentration of transthyretin (3.6 μM), under conditions where transthyretin amyloid fibril formation is maximal (pH 4.4). [3] This compound (viz 200 μM) produces a near complete collapse of the holding current at −50 mV, mirroring the effect of removal of extracellular Ca2+. It inhibits recombinant human TRPM2 (hTRPM2) as well as currents activated by intracellular ADP-ribose in the CRI-G1 rat insulinoma cell line. It antagonises ADP-ribose activated currents in the rat insulinoma cell line CRI-G1 in concentration- and pH-dependent kinetics manner. [4] It reversibly inhibits (IC50 = 13.8 μM) DAPs and phasic firing with a similar time course in rat supraoptic neurones, but has no significant effects (P > 0.05) on membrane potential, spike threshold and input resistance, nor on the frequency and amplitude of spontaneous synaptic potentials. [5]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/15275834/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12456832/

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