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Flunixin Meglumin

现货
Catalog No.
B1445
环氧合酶抑制剂
组合的产品项目
规格价格库存 数量
1g
¥ 1,140.00
现货
5g
¥ 3,800.00
Ship with 10-15 days
10mM (in 1mL DMSO)
¥ 500.00
现货

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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.

Chemical Properties

StorageStore at -20°C
M.Wt491.46
Cas No.42461-84-7
FormulaC14H11F3N2O2.C7H17NO5
Solubility≥24.55mg/mL in DMSO
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
SDFDownload SDF
Canonical SMILESCC1=C(C=CC=C1NC2=C(C=CC=N2)C(=O)O)C(F)(F)F.CNCC(C(C(C(CO)O)O)O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

犬多形核白细胞

溶解方法

在DMSO中的溶解度> 24.6mg/mL。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

10-4 M,37°C预孵育15分钟

应用

Flunixin Meglumin是leukotriene-B4诱导的犬多形核白细胞迁移的有效抑制剂。Flunixin Meglumin在狗中的部分抗炎作用可归因于其对多形核白细胞募集的抑制。

动物实验[1]:

动物模型

比格犬

剂量

1 mg/kg,静脉注射

应用

在狗中,Flunixin Meglumin在1小时时几乎完全消除了LTB4的反应,并且在24小时仍具有显著抑制活性。Flunixin Meglumin在狗中的部分抗炎作用可归因于对多形核白细胞募集的抑制。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

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.

质量控制

化学结构

Flunixin Meglumin