| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Cyclooxygenase (COX) - non-selective COX inhibitor.[1]
Flurbiprofen Axetil targets cyclooxygenase (COX) enzymes, both COX-1 and COX-2, which are involved in the conversion of arachidonic acid to prostaglandins. By inhibiting these enzymes, it reduces the production of pro-inflammatory prostaglandins, thereby alleviating pain and inflammation. |
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| ln Vitro |
In vitro, flurbiprofen axetil inhibits COX activity. It also inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. It demonstrates potency against the Ebola virus with AC50 values of 1778.3 nM and 1.778 µM in screening assays.
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| ln Vivo |
In patients undergoing open colorectal surgery, perioperative intravenous administration of Flurbiprofen Axetil (1 mg·kg⁻¹ iv 30 min before and 6 h after skin incision) combined with thoracic epidural anesthesia and postoperative PCEA significantly accelerated return of bowel function: time to first flatus 63±16 h vs 75±11 h in control (P=0.01); time to first bowel movement 87±23 h vs 105±19 h in control (P=0.008).[1]
Postoperative pain scores during coughing were significantly lower in the Flurbiprofen Axetil group at 1, 2, 4, 8, and 24 h postoperatively (P<0.001 at each time point), while resting VAS scores showed no significant difference between groups.[1] Plasma IL-6 levels were significantly lower in the Flurbiprofen Axetil group at end of surgery (33.03±7.53 vs 39.86±5.54 pg·mL⁻¹, P=0.002), at 6 h (55.28±6.15 vs 62.93±9.12 pg·mL⁻¹, P=0.004), and at 24 h (19.38±5.22 vs 24.61±5.84 pg·mL⁻¹, P=0.005) postoperatively compared to control.[1] Plasma IL-8 levels were significantly lower in the Flurbiprofen Axetil group at end of surgery (39.37±8.06 vs 47.86±8.45 pg·mL⁻¹, P=0.002), at 6 h (28.03±4.44 vs 31.38±4.78 pg·mL⁻¹, P=0.027), and at 24 h (14.67±4.75 vs 18.08±3.48 pg·mL⁻¹, P=0.013) postoperatively compared to control.[1] Plasma IL-10 levels were significantly higher in the Flurbiprofen Axetil group at 6 h postoperatively (31.65±6.20 vs 15.90±6.96 pg·mL⁻¹, P=0.009).[1] At 24 h postoperatively, total leukocyte count was significantly lower in the Flurbiprofen Axetil group (9.1±1.02 vs 10.8±1.88 ×10⁶ L⁻¹, P=0.001), and body temperature was also lower (37.6±0.38 vs 37.9±0.39 °C, P=0.006) compared to control.[1] In vivo, flurbiprofen axetil is used to treat pain, inflammation, and fever. As a prodrug, it is converted to the active flurbiprofen, which exerts its effects systemically. It has anti-inflammatory effects in various animal models of inflammation. |
| Enzyme Assay |
Cell-free COX inhibition assays are performed using purified COX-1 and COX-2 enzymes and arachidonic acid as substrate. Flurbiprofen axetil or its active metabolite flurbiprofen is incubated with the enzyme, and the production of prostaglandins (e.g., PGE2) is measured using ELISA or radiometric methods to determine the IC50.
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| Cell Assay |
In vitro cellular assays use cell lines such as macrophages or cancer cells. Cells are treated with flurbiprofen axetil, and the production of prostaglandins is measured to assess COX inhibition. The effect on cell proliferation and migration is studied in cancer cells to evaluate its anti-metastatic potential.
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| Animal Protocol |
Flurbiprofen Axetil was administered intravenously at a dose of 1 mg·kg⁻¹, 30 min before skin incision and again six hours after skin incision. The control group received an equal volume of intralipid (placebo). All patients received combined epidural/general anesthesia and postoperative patient-controlled epidural analgesia (PCEA) with morphine (0.025 mg·mL⁻¹) and ropivacaine (0.125%) in 200 mL 0.9% sodium chloride (bolus 2 mL, lockout 20 min, background infusion 3 mL·hr⁻¹). Peripheral venous blood samples were collected before FA infusion, at end of surgery, and 6 h and 24 h postoperatively. Plasma cytokines (IL-6, IL-8, IL-10) were measured by ELISA. Bowel function (time to first flatus and first bowel movement), pain scores (VAS at rest and during coughing), leukocyte count, and body temperature were recorded.[1]
In vivo efficacy is evaluated in animal models of inflammation, such as the carrageenan-induced paw edema model in rats. Flurbiprofen axetil is administered orally or via injection, and paw volume is measured to assess its anti-inflammatory effects. It is also studied in xenograft models of breast cancer to evaluate its anti-metastatic activity. |
| ADME/Pharmacokinetics |
Flurbiprofen Axetil (C19H19FO4) has a molecular weight of 330.35 g/mol. It is a prodrug of flurbiprofen. It is under investigation in clinical trial NCT02043366. Storage conditions include 4°C, sealed, away from moisture and light; in solvent at -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
No specific toxicity data (e.g., LD50, organ toxicity) were reported. The incidence of postoperative nausea and vomiting was similar between groups (nausea: 7 vs 8; vomiting: 5 vs 6). No patient suffered any adverse effects related to Flurbiprofen Axetil.[1]
The toxicity of flurbiprofen axetil is similar to other NSAIDs, including gastrointestinal irritation, ulceration, and bleeding due to COX-1 inhibition. Renal and cardiovascular effects may also occur. As a prodrug, it is designed to improve tolerability while maintaining efficacy. |
| References | |
| Additional Infomation |
Flurbiprofen ester is an organic molecular entity. Flurbiprofen ester is currently being investigated in the clinical trial NCT02043366 (Effect of butorphanol combined with flurbiprofen ester in preventing remifentanil-induced hyperalgesia in patients).
Flurbiprofen Axetil is a non-selective COX inhibitor formulated as lipid microspheres with high affinity to inflammatory tissues. Its elimination half-life is approximately 6 hours. The study demonstrated that perioperative intravenous FA combined with thoracic epidural anesthesia and PCEA may be a potential therapeutic strategy in fast-track rehabilitation programs for colorectal surgery, by reducing pro-inflammatory cytokines (IL-6, IL-8), increasing anti-inflammatory cytokine (IL-10), and accelerating bowel function recovery without increasing side effects.[1] Flurbiprofen Axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent. It is a prodrug of flurbiprofen. It inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. It has demonstrated antiviral properties against Ebola virus. |
| Exact Mass |
330.126
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|---|---|
| CAS # |
91503-79-6
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| PubChem CID |
3395
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| Appearance |
Colorless to off-white ointment
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
424.3±40.0 °C at 760 mmHg
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| Flash Point |
203.0±22.2 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.529
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| LogP |
4.53
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
24
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| Complexity |
433
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ALIVXCSEERJYHU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H19FO4/c1-12(19(22)24-14(3)23-13(2)21)16-9-10-17(18(20)11-16)15-7-5-4-6-8-15/h4-12,14H,1-3H3
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| Chemical Name |
1-acetyloxyethyl 2-(3-fluoro-4-phenylphenyl)propanoate
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| Synonyms |
Ropion RopiopnFlurbiprofen Axetil Lipfen LFP-83
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO : ~250 mg/mL (~756.77 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00725218 | COMPLETED | Drug: Saline Drug: Flurbiprofen Axetil |
Postoperative Pain | Nanjing Medical University | 2008-05 | Phase 4 |
| NCT03200600 | TERMINATED | Drug: Dexamethasone Drug: Normal saline Drug: Flurbiprofen axetil Drug: Lipid microsphere |
Flubiprofen Axetil Carcinoma, Non-Small-Cell Lung Delirium Dexamethasone Surgery--Complications |
Peking University First Hospital | 2017-08-02 | Phase 4 |
| NCT03422887 | COMPLETED | Drug: Nalbuphine Drug: Flurbiprofen Axetil Drug: Nalbuphine and Flurbiprofen Axetil |
Anesthesia Pain Surgery |
Sun Yat-sen University | 2018-01-18 | Not Applicable |
| NCT04611763 | UNKNOWN STATUS | Drug: Flurbiprofen axetil preoperatively Drug: Flurbiprofen axetil postoperatively |
Flurbiprofen Axetil Perioperative Sleep Quality Postoperative Inflammatory Markers Postoperative Pain Preemptive Analgesia |
Beijing Friendship Hospital | 2021-09-01 | Phase 1 |
| NCT04128410 | UNKNOWN STATUS | Flurbiprofen Axetil Aged Anesthesia, Spinal Cerebrospinal Fluid |
Yi Feng, MD | 2019-10 |
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