Flurbiprofen axetil
Based on 1 Customer Validation
Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.34%
- CAS 番号: 91503-79-6
- 分子式: C19H19FO4
- 分子量:330.35
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
生物活性
製品説明
IC50 & Target
[1]|
COX |
体外実験
Flurbiprofen axetil (0-160 nM, 1-6 days) does not affect the proliferation and activity, but inhibits migration and invasion in BT-549 and MDA-MB-231 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT-549 and MDA-MB-231 cells
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Concentration:0 nM, 40 nM, 80 nM, 160 nM
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Incubation Time:24 h
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Result:Inhibited the migration and invasion, and 80 nM was the most appropriate concentration to use.
体内実験
Flurbiprofen axetil (10 mg/kg, i.p., once every two days, 28 days) inhibits breast cancer metastasis via inhibiting MEK/ERK signaling pathway in nude mice model[2].
Flurbiprofen axetil (10 mg/kg, i.v., once) could promote a neuroprotective effect by, or in part, activation of PPAR-γ after focal cerebral ischemia in rat[3].
Flurbiprofen axetil (5-10 mg/kg, i.v., once) protects the brain from cerebral I/R injury through reducing inflammation and brain edema in global cerebral ischemia male SD rat[4].
Flurbiprofen axetil (10 mg/kg, i.v., once) can reduce the inflammatory response and cognitive function through the AMPKα/NF-κB signaling pathway.in formalin-induced MCI SD rat model[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:EIU rabbit model [1]
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Dosage:0.1 g/100 mL
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Administration:drops into the eyes, 2 times/day, 24 h
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Result:Reduce inflammatory response and leukocyte counts and PGE2 levels, reduce iris and retinal disorder and inflammatory cell infiltration.
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Animal Model:Breast cancer metastasis (1 × 106 MDA-MB-231-luc cells/100 µL, i.v.) nude mice (Female Balb/c, 6 weeks) model[2]
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Dosage:10 mg/kg
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Administration:i.p., once every two days, 28 days
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Result:Inhibited the expression of CD44 and VCAM-1, inhibited the metastasis. Inhibited the expression levels of key EMT markers (particularly N-cadherin and vimentin) without affecting proteins involved in the PI3K/AKT signaling pathway, Wnt/β-catenin signaling pathway, Janus kinase/STAT3 signaling pathway, and transforming growth factor-β/Smad signaling pathway. Inhibited the phosphorylation of MEK/ERK signaling pathway proteins and ERK phosphorylation.
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Animal Model:tMCAO male SD rat (8-12 weeks old, 280-320 g)[3]
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Dosage:10 mg/kg
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Administration:i.v., once
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Result:Reduced neurological deficit score, reduced infarct volume percentage.
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Animal Model:Global cerebral ischemia male SD rat (300-350 g) model[3]
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Dosage:5 mg/kg, 10 mg/kg
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Administration:i.v., once
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Result:Reduced neurological deficit score. Reduced cerebral I/R-induced neuronal damage, reduced cell apoptosis, TUNEL positive cells, cleaved caspase-3 protein expression. Reduces AQP4 and AQP9 mRNA expressions, reduces TXB2 and TXB2/6-keto-PGF1α in discrete cortex. Decreases cerebral I/R-induced inflammation in hippocampus, reduced serum TNF-α, IL-1β and ICAM-1 and NF-κB mRNA expressions.
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Animal Model:Formalin-induced MCI SD rat (male, 250-300 g, 16-17 weeks old) model[3]
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Dosage:10 mg/kg
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Administration:i.v., once
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Result:Relieved inflammatory pain induced by formalin injection, alleviated the effect on the cognitive function, reduced the effect on neuronal damage, decreased levels of TNF-α and IL-6 in the hippocampus. Inhibited NF-κB p65 by activating AMPKα.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 91503-79-6
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性状 Oil
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分子量 330.35
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分子式 C19H19FO4
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Color Colorless to off-white
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SMILES
O=C(OC(OC(C)=O)C)C(C)C1=CC=C(C2=CC=CC=C2)C(F)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
体外:
DMSO : 250 mg/mL (756.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Shen J, et al. Novel NSAIDs ophthalmic formulation: flurbiprofen axetil emulsion with low irritancy and improved anti-inflammation effect. Int J Pharm. 2011 Jun 30;412(1-2):115-22. [Content Brief]
[2]. Zhu Y, et al. Flurbiprofen axetil is involved in basal-like breast cancer metastasis via suppressing the MEK/ERK signaling pathway. Cell Biol Int. 2025 Jan;49(1):68-78. [Content Brief]
[3]. Liu JL, et al. Flurbiprofen axetil promotes neuroprotection by activation of cerebral peroxisome proliferator-activated receptor gamma after focal cerebral ischemia in rats. Chin Med J (Engl). 2012 Oct;125(20):3719-24. [Content Brief]
[4]. Wu H, et al. Flurbiprofen axetil attenuates cerebral ischemia/reperfusion injury by reducing inflammation in a rat model of transient global cerebral ischemia/reperfusion. Biosci Rep. 2018 Jul 6;38(4):BSR20171562. [Content Brief]
[5]. Huang L, et al. Flurbiprofen axetil alleviates the effect of formalin-induced inflammatory pain on the cognitive function of rats with mild cognitive impairment through the AMPKα/NF-κB signaling pathway. Ann Transl Med. 2022 Nov;10(22):1210. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0271 mL | 15.1355 mL | 30.2709 mL | 75.6773 mL |
| 5 mM | 0.6054 mL | 3.0271 mL | 6.0542 mL | 15.1355 mL | |
| 10 mM | 0.3027 mL | 1.5135 mL | 3.0271 mL | 7.5677 mL | |
| 15 mM | 0.2018 mL | 1.0090 mL | 2.0181 mL | 5.0452 mL | |
| 20 mM | 0.1514 mL | 0.7568 mL | 1.5135 mL | 3.7839 mL | |
| 25 mM | 0.1211 mL | 0.6054 mL | 1.2108 mL | 3.0271 mL | |
| 30 mM | 0.1009 mL | 0.5045 mL | 1.0090 mL | 2.5226 mL | |
| 40 mM | 0.0757 mL | 0.3784 mL | 0.7568 mL | 1.8919 mL | |
| 50 mM | 0.0605 mL | 0.3027 mL | 0.6054 mL | 1.5135 mL | |
| 60 mM | 0.0505 mL | 0.2523 mL | 0.5045 mL | 1.2613 mL | |
| 80 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9460 mL | |
| 100 mM | 0.0303 mL | 0.1514 mL | 0.3027 mL | 0.7568 mL |