Flurbiprofen axetil solution
Flurbiprofen axetil solution is mainly composed of Flurbiprofen axetil (HY-101481). 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.
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- CAS No.: 91503-79-6
- Formule: C19H19FO4
- Masse moléculaire:330.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
[1]|
COX |
In Vitro
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.
In Vivo
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.
Chemical Information
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CAS No. 91503-79-6
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Masse moléculaire 330.35
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Formule C19H19FO4
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SMILES
O=C(C(C1=CC=C(C(F)=C1)C2=CC=CC=C2)C)OC(C)OC(C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Flurbiprofen axetil solution
- 91503-79-6
- COX
- Apoptosis
- MEK
- ERK
- PPAR
- AMPK
- NF-κB
- Interleukin Related
- TNF Receptor
- STAT
- Wnt
- Cyclooxygenase
- Mitogen-activated protein kinase kinase
- MAPKK
- MAP2K
- Extracellular signal regulated kinases
- Peroxisome proliferator-activated receptors
- AMP-activated protein kinase
- Nuclear factor-κB
- Nuclear factor-kappaB
- IL
- Tumor Necrosis Factor Receptor
- TNFR
- Inhibitor
- MEK/ERK
- AMPKα/NF-κB
- MCI SD rat model
- BT-549 cells
- MDA-MB-231 cells
- tMCAO
- EIU rabbit model
- inhibitor
- inhibit