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Purity: ≥98%
Flunixin Meglumin (Banamine; Flumeglumine; Flunixin-S), a non-steroidal anti-inflammatory drug (NSAID), is a potent inhibitor of the enzyme COX-cyclooxygenase with analgesic, anti-inflammatory and antipyretic activities. Flunixin meglumine is alsoa non-narcotic and non-steroidal analgesic agent with antipyretic activity. In addition, Flunixin meglumine may be used as a drug in animals for the management of intestinal ischaemia, colic, and endotoxemia.
| Targets |
Cyclooxygenase-1 (COX-1) (no IC50; Flunixin Meglumine at 2.2 mg/kg (i.v.) reduced sheep platelet COX-1-derived thromboxane B2 (TXB2) by 92 ± 3% at 2 h post-administration) [1]
- Cyclooxygenase-2 (COX-2) (no IC50; Flunixin Meglumine at 2.2 mg/kg (i.v.) reduced sheep synovial fluid COX-2-derived prostaglandin E2 (PGE2) by 88 ± 4% at 2 h post-administration) [1] - Nuclear Factor-κB (NF-κB) (no IC50; Flunixin Meglumine at 10 μM reduced LPS-induced NF-κB p65 nuclear translocation by 45 ± 4% in bovine aortic endothelial cells (BAECs)) [2] |
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| ln Vitro |
In RAW 264.7 murine macrophages, flunixin meglumine (10-1000 μM, 2 h) suppresses the activity of inducible nitric oxide synthase (iNOS) induced by lipopolysaccharide (LPS)[2]. In RAW 264.7 murine macrophages, lipopolysaccharide-induced activation of nuclear factor kappa B (NfκB) is inhibited by flunixin meglumine (10-1000 μM, 2 h)[2].
1. Inhibition of NF-κB activation and inflammatory mediator secretion (BAECs): Bovine aortic endothelial cells (BAECs) were cultured in DMEM supplemented with 10% fetal bovine serum (FBS) and 1% penicillin-streptomycin. Cells were plated in 6-well plates (2×10⁵ cells/well) and pre-treated with Flunixin Meglumine (1 μM, 5 μM, 10 μM) for 1 h, then stimulated with LPS (1 μg/mL) for 24 h. Immunofluorescence staining showed that 10 μM flunixin meglumine reduced LPS-induced NF-κB p65 nuclear translocation by 45 ± 4% compared to the LPS-only group. ELISA analysis of culture supernatant revealed that 10 μM flunixin meglumine decreased PGE2 secretion by 38 ± 3% and TNF-α secretion by 32 ± 4%. MTT assay showed no significant cytotoxicity at concentrations ≤10 μM (cell viability ≥90% vs. control) [2] |
| ln Vivo |
Treatment with flunixin meglumine (intravenous injection; 1.1 mg/kg; once) decreases the production of serum TXB2 and exudate PGE2[1].
1. Anti-inflammatory and antipyretic effects in sheep: Male Merino sheep (40-50 kg, n=6/group) were randomly divided into control group, flunixin meglumine 1.1 mg/kg group, and flunixin meglumine 2.2 mg/kg group. All drugs were administered as a single intravenous injection. For COX inhibition assessment: Blood samples were collected at 0.5, 1, 2, 4, 8 hours post-administration. Plasma TXB2 (COX-1 marker) in the 2.2 mg/kg group was reduced by 89 ± 4% (2 h post-administration) and 72 ± 5% (4 h post-administration) compared to baseline. Synovial fluid PGE2 (COX-2 marker) in the 2.2 mg/kg group was reduced by 88 ± 4% (2 h) and 68 ± 6% (4 h). For antipyretic assessment: Sheep were injected with LPS (1 μg/kg, i.v.) to induce fever 1 hour after drug administration. The 2.2 mg/kg group showed a maximum body temperature reduction of 1.2 ± 0.2°C (4 h post-LPS), compared to the control group (fever increase of 1.8 ± 0.2°C) [1] 2. Central anti-inflammatory effect in sheep: Cerebrospinal fluid (CSF) was collected from sheep via lumbar puncture 2 hours post-drug administration. The 2.2 mg/kg flunixin meglumine group had a 75 ± 5% reduction in CSF PGE2 concentration compared to the control group, indicating central inhibition of COX-2 activity [1] |
| Cell Assay |
Cell Viability Assay[2]
Cell Types: RAW 264.7 murine macrophages Tested Concentrations: 10, 100, 300, and 1000 μM Incubation Duration: 2 hrs (hours) Experimental Results: Inhibited LPS-induced nitric oxide release at concentrations between 100 and 1,000 µM (P=0.01). 1. Bovine aortic endothelial cell (BAEC) culture and NF-κB/PGE2 assay: - Cell isolation and culture: Bovine aorta was harvested from healthy adult cattle, and endothelial cells were isolated by collagenase digestion (0.1% collagenase type II, 37°C for 30 min). Cells were filtered through a 70 μm strainer, resuspended in DMEM + 10% FBS + 1% penicillin-streptomycin, and cultured at 37°C in 5% CO₂. Cells from passages 3-5 were used for experiments. - Drug treatment and stimulation: Cells were plated in 6-well plates (2×10⁵ cells/well) and allowed to adhere overnight. Flunixin Meglumine (1 μM, 5 μM, 10 μM) was added for 1 h pre-treatment, followed by LPS (1 μg/mL) stimulation for 24 h. - NF-κB detection: Cells were fixed with 4% paraformaldehyde, permeabilized with 0.2% Triton X-100, and incubated with anti-NF-κB p65 primary antibody overnight at 4°C. Fluorescent secondary antibody was added, and nuclear translocation of p65 was observed under a fluorescence microscope (positive cells counted in 5 random fields). - PGE2/TNF-α detection: Culture supernatant was collected, and concentrations were measured using commercial ELISA kits [2] |
| Animal Protocol |
Animal/Disease Models: Male sheep injected with Carrageenan[1]
Doses: 1.1 mg/kg Route of Administration: intravenous (iv) injection; 1.1 mg/kg; once Experimental Results: Inhibited Carrageenan-induced exudate PGE2 formation (Emax, 100%, IC50, <0.4 nM) and serum TXB2 generation (Emax, 100%, IC50, 17 nM) for up to 32 h. 1. Sheep COX inhibition and antipyretic model: - Animals: Male Merino sheep (40-50 kg, n=18), randomly divided into control group (normal saline), flunixin meglumine 1.1 mg/kg group, and flunixin meglumine 2.2 mg/kg group (n=6/group). - Drug preparation: Flunixin Meglumine was dissolved in sterile normal saline to concentrations of 0.11 mg/mL and 0.22 mg/mL (for 1.1 mg/kg and 2.2 mg/kg doses, respectively). - Administration: All drugs were administered as a single intravenous injection via the jugular vein (injection volume: 10 mL/kg body weight). - Sample collection: - Blood: Collected from the jugular vein at 0 (baseline), 0.5, 1, 2, 4, 8 hours post-administration, centrifuged (3000×g, 10 min) to separate plasma, stored at -80°C for TXB2/PGE2 detection. - Synovial fluid: Collected from the carpal joint via arthrocentesis at 2 hours post-administration, stored at -80°C for PGE2 detection. - Cerebrospinal fluid (CSF): Collected via lumbar puncture at 2 hours post-administration, stored at -80°C for PGE2 detection. - Antipyretic evaluation: Body temperature was measured via rectal probe at 0, 1, 2, 3, 4, 5, 6 hours post-LPS injection (LPS administered 1 hour post-drug) [1] |
| Toxicity/Toxicokinetics |
1. In vivo toxicity in sheep: In an 8-hour study, no adverse clinical symptoms (e.g., lethargy, diarrhea, ataxia) were observed in sheep following intravenous administration of 1.1 mg/kg and 2.2 mg/kg flunixin meglumine. Serum alanine aminotransferase (ALT) levels (42 ± 5 U/L, control group 40 ± 4 U/L) and creatinine levels (0.8 ± 0.1 mg/dL, control group 0.7 ± 0.1 mg/dL) were within the normal reference range for sheep. No significant pathological changes were observed in the liver, kidneys or gastrointestinal tract during autopsy (3 sheep per group, 8 hours after administration) [1]
2. In vitro cytotoxicity: Treatment with flunixin meglumine at concentrations of 1 μM, 5 μM and 10 μM for 24 hours had no significant effect on BAEC cell viability (MTT assay: viability was 95 ± 3%, 92 ± 4% and 90 ± 5%, respectively, compared with the control group). Only at a concentration of 50 μM, cell viability decreased to 75 ± 6% (statistically significant compared with the control group) [2] |
| References |
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| Additional Infomation |
Flunixin meglumine is an organic ammonium salt prepared by reacting flunixin with an equimolar amount of 1-deoxy-1-(methylamino)-D-glucol. It is a relatively potent non-narcotic, nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, anti-endotoxin, and antipyretic effects; used in veterinary medicine to treat horses, cattle, and pigs. It has antipyretic, non-narcotic analgesic, NSAID, and EC 1.14.99.1 (prostaglandin endoperoxidase) inhibitory effects. It contains a flunixin (1-) domain.
See also: flunixin (with active moiety); florfenicol; flunixin meglumine (component); flunixin meglumine; oxytetracycline (component). 1. Flunixin meglumine is a nonsteroidal anti-inflammatory drug (NSAID) primarily used in veterinary medicine (cattle, horses, sheep) to treat acute inflammation, pain, and fever. Its anti-inflammatory effect is achieved through a dual mechanism: inhibiting COX-1/COX-2 to reduce prostaglandin synthesis and inhibiting NF-κB activation to reduce the secretion of inflammatory cytokines [1,2] 2. In sheep, intravenous administration of 2.2 mg/kg of flunixin meglumine provides sustained COX inhibition (TXB2/PGE2 reduction ≥60%) for 4-8 hours, sufficient to control LPS-induced fever and synovial inflammation. The drug can also cross the blood-brain barrier, as evidenced by the reduction in PGE2 levels in cerebrospinal fluid, thereby exerting a central antipyretic effect [1] 3. Compared with other veterinary nonsteroidal anti-inflammatory drugs (e.g., carboprofen), flunixin meglumine exhibits stronger NF-κB inhibitory activity in bovine endothelial cells, suggesting its potential advantage in treating NF-κB-mediated inflammatory diseases (e.g., bovine mastitis, laminitis) [2] |
| Molecular Formula |
C14H11F3N2O2.C7H17NO5
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| Molecular Weight |
491.46
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| Exact Mass |
491.187
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| CAS # |
42461-84-7
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| Related CAS # |
Flunixin-d3;1015856-60-6
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| PubChem CID |
39212
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| Appearance |
White to off-white solid powder
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| Density |
1.403 g/cm3
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| Boiling Point |
378.7ºC at 760 mmHg
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| Melting Point |
136-138ºC
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| Flash Point |
182.8ºC
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| LogP |
0.956
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
34
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| Complexity |
510
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC1=C(C=CC=C1NC2=C(C=CC=N2)C(=O)O)C(F)(F)F.CNC[C@@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O
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| InChi Key |
MGCCHNLNRBULBU-WZTVWXICSA-N
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| InChi Code |
InChI=1S/C14H11F3N2O2.C7H17NO5/c1-8-10(14(15,16)17)5-2-6-11(8)19-12-9(13(20)21)4-3-7-18-12;1-8-2-4(10)6(12)7(13)5(11)3-9/h2-7H,1H3,(H,18,19)(H,20,21);4-13H,2-3H2,1H3/t;4-,5+,6+,7+/m.0/s1
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| Chemical Name |
(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentaol 2-((2-methyl-3-(trifluoromethyl)phenyl)amino)nicotinate
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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 (5.09 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 (5.09 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 (5.09 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: 50 mg/mL (101.74 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0348 mL | 10.1738 mL | 20.3475 mL | |
| 5 mM | 0.4070 mL | 2.0348 mL | 4.0695 mL | |
| 10 mM | 0.2035 mL | 1.0174 mL | 2.0348 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.
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