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Flunixin Meglumin potent cyclooxygenase inhibitor

Catalog No.B1445
Size Price Stock Qty
10mM (in 1mL DMSO)
$50.00
In stock
Evaluation Sample
$28.00
In stock
50mg
$50.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

Flunixin Meglumin

Protocol

Cell experiment [1]:

Cell lines

Canine polymorphonuclear leucocyte

Preparation method

The solubility of this compound in DMSO is >24.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10-4 M, pre-incubated for 15 min at 37°C

Applications

Flunixin Meglumin is a potent inhibitor on leukotriene-B4-directed migration of canine polymorphonuclear leucocyte. Part of the anti-inflammatory action of Flunixin Meglumin in dogs may be attributed to inhibition of polymorphonuclear leucocyte recruitment.

Animal experiment [1]:

Animal models

Beagle dogs

Dosage form

1 mg/kg, i.v.

Application

Flunixin Meglumin almost completely abolished the LTB4 response at 1 h, and still possessed significant inhibitory activity 24 h in dog. Part of the anti-inflammatory action of Flunixin Meglumin in dogs may be attributed to inhibition of polymorphonuclear leucocyte recruitment.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Strm H, Thomsen MK. Effects of non-steroidal anti-inflammatory drugs on canine neutrophil chemotaxis. J Vet Pharmacol Ther. 1990 Jun;13(2):186-91.

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Chemical Properties

Cas No. 42461-84-7 SDF Download SDF
Chemical Name (2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol;2-[2-methyl-3-(trifluoromethyl)anilino]pyridine-3-carboxylic acid
Canonical SMILES CC1=C(C=CC=C1NC2=C(C=CC=N2)C(=O)O)C(F)(F)F.CNCC(C(C(C(CO)O)O)O)O
Formula C14H11F3N2O2.C7H17NO5 M.Wt 491.46
Solubility >24.6mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

IC50: A potent cyclooxygenase inhibitor with IC50 values of 1 nM.

Flunixin meglumine serves as a non-narcotic and non-steroidal analgesic agent with antipyretic activities. As a potent inhibitor of the enzyme cyclooxygenase, Flunixin meglumine has demonstrated a wide-spectrum of biological activities including anti-inflammation and pain-alleviating. Moreover, Flunixin meglumine could be applied as a drug in animals for the management of intestinal ischaemia, colic, and endotoxemia. [1]

In vitro: An in vitro whole blood model in feedlot calves was adopted to detect the activity of the anti-inflammatory agents Flunixin-meglumine (FLU), RS (±) Carprofen (CPF) and S (+) CPF. The drugs all exhibited inhibitory activity on COXs, with an order of FLU > S (+) CPF > RS (±) CPF in their potency. This finding indicated that FLU was a nonselective suppressorr of bovine COXs, whereas RS (±) CPF and S (+) CPF selectively inhibited COX-2 isoenzyme. [2]

In vivo: Findings from mice, rats and monkeys suggested Flunixin meglumine as a potent non-narcotic analgesic agent after parenteral administration. After being subcutaneous administered, this agent showed higher efficacy than pentazocine, meperidine and codeine in the rat yeast paw test. Intramuscular administration and subcutaneous administration of Flunixin meglumine had similar effects. Moreover, orally administered Flunixin meglumine also exerted analgesic and anti-inflammatory activities. Based on mice abdominal constriction test, flunixin meglumine had comparable efficacy to pentazocine and was more potent than meperidine and codeine. In primates, 10 mg/kg flunixin meglumine showed an equal efficacy to that of 0.3 mg/kg morphine. [1]

Clinical trials: Flunixin meglumine, in a dosage of 1.0 mg/kg bwt, was studied in a blind Multi-Centre clinical trial in 152 horses with abdominal pain. Significant differences were noted in kicking, pawing, head and body movement and attitude between the horses receiving flunixin meglumine and control. Moreover, compared with detomidin, Flunixin meglumine provided significantly less analgesia. [3]

References:
[1]Ciofalo VB, Latranyi MB, Patel JB and Taber RI.  Flunixin meglumine: a non-narcotic analgesic. J Pharmacol Exp Ther. 1977 Mar; 200(3): 501-7.
[2]Miciletta M, Cuniberti B, Barbero R and Re G.  In vitro enantioselective pharmacodynamics of Carprofen and Flunixin-meglumine in feedlot cattle. J Vet Pharmacol Ther. 2014 Feb; 37(1): 43-52.
[3] Jochle W, Moore JN, Brown J, Baker GJ, Lowe JE, Fubini S, Reeves MJ, Watkins JP and White NA.  Comparison of detomidine, butorphanol, flunixin meglumine and xylazine in clinical cases of equine colic. Equine Vet J Suppl. 1989 Jun; (7): 111-6.