氟比洛芬（2-20 nM；12-48 小时）以浓度和时间依赖性方式强烈抑制 SW620 细胞的生长 [1]。氟比洛芬 (10 nM) 会降低 COX-2 的表达 24 小时 [1]。通过阻断 COX-2，氟比洛芬（10 nM；24 小时）可减少炎症因子的表达 [1]。通过阻断 COX-2，氟比洛芬（10 nM；24 小时）可促进结直肠癌细胞凋亡 [1]。细胞增殖实验[1]

在肾上腺切除术的大鼠中，氟比洛芬（0.3-4.8 mg/kg；口服；4-5 剂）表现出立竿见影的抗炎作用 [2]。在高脂肪饮食的小鼠中，氟比洛芬（10 mg/kg；腹腔注射；每天；持续 6 天）可减少肥胖[3]。

细胞增殖实验 [1]
细胞类型： SW620 细胞
测试浓度： 2 nM、4 nM、10 nM、20 nM
孵化持续时间：12小时、24小时、48小时
实验结果：抑制结直肠癌癌细胞增殖。

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蛋白质印迹分析[1]
细胞类型： SW620 细胞
测试浓度： 10 nM
孵育时间：24小时
实验结果：COX-2的蛋白和mRNA水平显着降低。

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RT-PCR[1]
细胞类型： SW620 细胞
测试浓度： 10 nM
孵育时间：24小时
实验结果：COX-2 mRNA表达水平降低细胞凋亡分析[1]
细胞类型： strong> SW620 细胞
测试浓度： 10 nM
孵育时间： 24 小时
实验结果：< Bcl2的表达显着减少，Bax和cleaved-caspase3的表达显着增加，但对总caspase-3没有影响。

Animal/Disease Models: Rat[2]
Doses: 0.3 mg/kg, 0.6 mg/kg, 1.2 mg/kg, 2.4 mg/kg, 4.8 mg/kg
Route of Administration: po (po (oral gavage)) 4-5 times
Experimental Results: Inhibition of acute inflammation.

Absorption, Distribution and Excretion
Fluribiprofen is rapidly and almost completely absorbed following oral administration. Peak plasma concentrations are reached 0.5 - 4 hours after oral administration.
Flurbiprofen is poorly excreted into human milk. Following dosing with flurbiprofen, less than 3% of flurbiprofen is excreted unchanged in the urine, with about 70% of the dose eliminated in the urine as parent drug and metabolites. Renal elimination is a significant pathway of elimination of flurbiprofen metabolites.
14 L [Normal Healthy Adults]
12 L [Geriatric Arthritis Patients]
10 L [End Stage Renal Disease Patients]
14 L [Alcoholic Cirrhosis Patients]
0.12 L/kg

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Metabolism / Metabolites
Hepatic. Cytochrome P450 2C9 plays an important role in the metabolism of flurbiprofen to its major metabolite, 4’-hydroxy-flurbiprofen. The 4’-hydroxy-flurbiprofen metabolite showed little anti-inflammatory activity in animal models of inflammation.
Hepatic. Cytochrome P450 2C9 plays an important role in the metabolism of flurbiprofen to its major metabolite, 4’-hydroxy-flurbiprofen. The 4’-hydroxy-flurbiprofen metabolite showed little anti-inflammatory activity in animal models of inflammation.
Route of Elimination: Flurbiprofen is poorly excreted into human milk. Following dosing with flurbiprofen, less than 3% of flurbiprofen is excreted unchanged in the urine, with about 70% of the dose eliminated in the urine as parent drug and metabolites. Renal elimination is a significant pathway of elimination of flurbiprofen metabolites.
Half Life: R-flurbiprofen, 4.7 hours; S-flurbiprofen, 5.7 hours

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Biological Half-Life
R-flurbiprofen, 4.7 hours; S-flurbiprofen, 5.7 hours

Hepatotoxicity
Prospective studies show that mild elevations in serum aminotransferase levels can occur in up to 15% of patients taking flurbiprofen, but these are generally transient, mild and asymptomatic, often resolving even with drug continuation. Marked aminotransferase elevations (>3 fold elevated) occur in
Likelihood score: C (probable rare cause of clinically apparent liver injury).

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Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Because of the low levels of flurbiprofen in breastmilk and its short half-life it is unlikely to adversely affect the breastfed infant, especially if the infant is older than 2 months.
Maternal use of flurbiprofen eye drops would not be expected to cause any adverse effects in breastfed infants. To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.
◉ Effects in Breastfed Infants
A retrospective medical record review in Taiwan compared the full-term breastfed infants of women who received acetaminophen (n = 348) to those who received flurbiprofen (n = 132) for postpartum analgesia after a vaginal birth. There was no statistically significant difference in the percentage of infants with hyperbilirubinemia between those whose mothers received flurbiprofen (0.76%) and those whose mothers received acetaminophen(2.01%).
A study of full-term, vaginally delivered breastfed neonates compared those whose mothers received acetaminophen (n = 348) to those whose mothers received flurbiprofen (n = 132) for postpartum pain. Seven (2%) newborns of acetaminophen users had hyperbilirubinemia and 1 (0.76%) newborn of the flurbiprofen users had hyperbilirubinemia. The differences was not statistically significant.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

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Protein Binding
> 99% bound, primarily to albumin. Binds to a different primary binding site on albumin than anticoagulants, sulfonamides and phenytoin.

[1]. Flurbiprofen suppresses the inflammation, proliferation, invasion and migration of colorectal cancer cells via COX2. Oncol Lett. 2020 Nov; 20(5): 132.

[2]. The pharmacology of 2-(2-fluoro-4-biphenylyl)propionic acid (flurbiprofen). A potent non-steroidal anti-inflammatory drug. Agents Actions. 1973 Nov;3(4):210-6.

[3]. Flurbiprofen ameliorated obesity by attenuating leptin resistance induced by endoplasmic reticulum stress. EMBO Mol Med, 2014.

Description
Flurbiprofen can cause developmental toxicity and female reproductive toxicity according to state or federal government labeling requirements.
Flurbiprofen is a monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain. It has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, an antipyretic and an EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor. It is a fluorobiphenyl and a monocarboxylic acid. It is functionally related to a propionic acid. It derives from a hydride of a biphenyl.
Flurbiprofen, a propionic acid derivative, is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity. Oral formulations of flurbiprofen may be used for the symptomatic treatment of rheumatoid arthritis, osteoarthritis and anklylosing spondylitis. Flurbiprofen may also be used topically prior to ocular surgery to prevent or reduce intraoperative miosis. Flurbiprofen is structurally and pharmacologically related to fenoprofen, ibuprofen, and ketoprofen.
Flurbiprofen is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of flurbiprofen is as a Cyclooxygenase Inhibitor.
Flurbiprofen is a nonsteroidal antiinflammatory drug (NSAID) used in treatment of mild-to-moderate pain and symptoms of chronic arthritis. Flurbiprofen has been linked to a low rate of serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury.
Flurbiprofen is a derivative of propionic acid, and a phenylalkanoic acid derivative of non-steroidal antiinflammatory drugs (NSAIDs) with analgesic, antiinflammatory and antipyretic effects. Flurbiprofen non-selectively binds to and inhibits cyclooxygenase (COX). This results in a reduction of arachidonic acid conversion into prostaglandins that are involved in the regulation of pain, inflammation and fever. This NSAID also inhibits carbonic anhydrase, thereby reducing the production of hydrogen and bicarbonate ions. Upon ocular administration, flurbiprofen may reduce bicarbonate ion concentrations leading to a decrease in the production of aqueous humor, thereby lowering intraocular pressure.
Flurbiprofen, a propionic acid derivative, is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity. Oral formulations of flurbiprofen may be used for the symptomatic treatment of rheumatoid arthritis, osteoarthritis and anklylosing spondylitis. Flurbiprofen may also be used topically prior to ocular surgery to prevent or reduce intraoperative miosis. Flurbiprofen is structurally and pharmacologically related to fenoprofen, ibuprofen, and ketoprofen.
An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.
See also: Flurbiprofen Sodium (has salt form); Flurbiprofen Axetil (is active moiety of).

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Drug Indication
Flurbiprofen tablets are indicated for the acute or long-term symptomatic treatment of rheumatoid arthritis, osteorarthritis and anklosing spondylitis. It may also be used to treat pain associated with dysmenorrhea and mild to moderate pain accompanied by inflammation (e.g. bursitis, tendonitis, soft tissue trauma). Topical ophthalmic formulations may be used pre-operatively to prevent intraoperative miosis.
FDA Label

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Mechanism of Action
Similar to other NSAIAs, the anti-inflammatory effect of flurbiprofen occurs via reversible inhibition of cyclooxygenase (COX), the enzyme responsible for the conversion of arachidonic acid to prostaglandin G2 (PGG2) and PGG2 to prostaglandin H2 (PGH2) in the prostaglandin synthesis pathway. This effectively decreases the concentration of prostaglandins involved in inflammation, pain, swelling and fever. Flurbiprofen is a non-selective COX inhibitor and inhibits the activity of both COX-1 and -2. It is also one of the most potent NSAIAs in terms of prostaglandin inhibitory activity.

C15H13FO2

244.2609

244.089

5104-49-4

Tarenflurbil;51543-40-9;Flurbiprofen-d3;1185133-81-6;Flurbiprofen-d5;215175-76-1;Flurbiprofen-13C,d3;2747917-55-9

3394

White to light yellow solid powder

1.2±0.1 g/cm3

376.2±30.0 °C at 760 mmHg

110-112 °C(lit.)

181.3±24.6 °C

0.0±0.9 mmHg at 25°C

1.568

4.11

37.3

1

3

3

18

286

0

SYTBZMRGLBWNTM-UHFFFAOYSA-N

InChI=1S/C15H13FO2/c1-10(15(17)18)12-7-8-13(14(16)9-12)11-5-3-2-4-6-11/h2-10H,1H3,(H,17,18)

2-(3-fluoro-4-phenylphenyl)propanoic acid

Cebutid, dl-Flurbiprofen; Ansaid, Froben, Flurbiprofen, Antadys

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 100 mg/mL (~409.40 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (10.23 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (10.23 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (10.23 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。