| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
The primary targets of Fenbufen are cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). By inhibiting COX enzymes, fenbufen reduces the synthesis of prostaglandins, which are key mediators of inflammation, pain, and fever. The compound has IC50 values of 3.9 µM for COX-1 and 8.1 µM for COX-2. Fenbufen also inhibits caspases (caspase-1, 3, 4, 5, 9). This dual mechanism of action contributes to its anti-inflammatory and analgesic effects.
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|---|---|
| ln Vitro |
The viability of apoptotic THP-1 cells treated with 25 μM nigericin can be increased by fenbufen (100-500 μM) [5].
In vitro, Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 µM and 8.1 µM, respectively. It is also a caspases (caspase-1, 3, 4, 5, 9) inhibitor. The compound's anti-inflammatory activity has been confirmed in various in vitro models. Its effects on prostaglandin synthesis and caspase activity have been demonstrated in cell-based assays. |
| ln Vivo |
Rats fed fenbufenme (1200 mg/kg) experience near-maximum suppression of prostaglandin release, although this does not result in stomach ulcers [6]. Heart hypertrophy is prevented by fenbufenmid (1200 mg/kg; oral; dietary; for 10 days) but not skeletal muscle hypertrophy [6].
In vivo, Fenbufen has strong activity in various animal models, including carrageenan-induced edema, UV erythema, and adjuvant-induced arthritis. It is used for the treatment of osteoarthritis, ankylosing spondylitis, and tendonitis. The compound is also used to relieve back pain, sprains, and fractures. Fenbufen is a non-steroidal anti-inflammatory drug (NSAID). |
| Enzyme Assay |
In vitro enzyme or receptor binding assays for Fenbufen involve measuring its inhibition of COX-1 and COX-2 enzymatic activity. The assay uses a purified COX enzyme and a substrate, such as arachidonic acid. The production of prostaglandins is measured using a colorimetric or fluorometric method. The compound is incubated with the enzyme and substrate at varying concentrations, and the IC50 is determined. Caspase inhibition is measured using fluorogenic substrates.
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| Cell Assay |
In vitro cell-based assays for Fenbufen are performed using various cell lines, such as macrophages or synoviocytes. Cells are treated with the compound, and the production of prostaglandins and inflammatory cytokines is measured by ELISA. The compound's effects on cell viability, proliferation, and apoptosis are also assessed. Caspase activity is measured using fluorogenic substrates.
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| Animal Protocol |
Animal/Disease Models: Male capped Lister rat [6]
Doses: 1200 mg/kg Route of Administration: po (po (oral gavage)) dietary, for 10 days Experimental Results: Dramatically diminished cardiac hypertrophy caused by clenbuterol (2mg/kg). In vivo animal experiments for Fenbufen are conducted using rodent models of inflammation, such as carrageenan-induced paw edema, UV erythema, and adjuvant-induced arthritis. The compound is administered orally or intraperitoneally, and inflammation and pain are assessed. These studies confirm the compound's efficacy as an anti-inflammatory and analgesic agent. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of Fenbufen indicate that it is orally active. The compound has a molecular weight of 254.28 and a molecular formula of C16H14O3. It has a purity of ≥98%. The compound is metabolized in the liver and excreted renally. Its half-life is approximately 10-12 hours. Fenbufen is highly protein-bound. Storage at -20°C is recommended.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for Fenbufen indicate that it is generally well-tolerated. Common side effects include gastrointestinal disturbances, such as nausea, vomiting, and diarrhea. The compound may also cause hepatotoxicity and nephrotoxicity. It should be used with caution in patients with a history of peptic ulcer disease, renal impairment, or hepatic impairment.
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| References |
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| Additional Infomation |
Fenbufen belongs to the biphenyl class of compounds and is a 4-oxomonocarboxylic acid. It is a nonsteroidal anti-inflammatory drug (NSAID). Fenbufen is primarily used to treat inflammation caused by osteoarthritis, ankylosing spondylitis, and tendinitis. It can also be used to relieve back pain, sprains, and fractures. Fenbufen is available in capsule and tablet forms, with brand names including Cepal, Cinopal, Cybufen, Lederfen, and Reugast. The mechanism of action of fenbufen is to inhibit the production of prostaglandins by cyclooxygenase, thereby reducing inflammation.
Other information: Fenbufen is also known as Lederfen, Cinopal, and Napanol. It is a non-steroidal anti-inflammatory drug (NSAID). The compound is used for the treatment of osteoarthritis, ankylosing spondylitis, and tendonitis. Its CAS number is 36330-85-5. |
| Molecular Formula |
C16H14O3
|
|---|---|
| Molecular Weight |
254.285
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| Exact Mass |
254.094
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| CAS # |
36330-85-5
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| Related CAS # |
Fenbufen-d9;1189940-96-2
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| PubChem CID |
3335
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
470.2±28.0 °C at 760 mmHg
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| Melting Point |
184-187ºC(lit.)
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| Flash Point |
252.3±20.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.585
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| LogP |
3.13
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
19
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| Complexity |
310
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZPAKPRAICRBAOD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14O3/c17-15(10-11-16(18)19)14-8-6-13(7-9-14)12-4-2-1-3-5-12/h1-9H,10-11H2,(H,18,19)
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| Chemical Name |
4-oxo-4-(4-phenylphenyl)butanoic acid
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| Synonyms |
Lederfen; Cinopal; Fenbufen
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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 |
| 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 : ~50 mg/mL (~196.63 mM)
H2O : ~0.67 mg/mL (~2.63 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.83 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9325 mL | 19.6626 mL | 39.3252 mL | |
| 5 mM | 0.7865 mL | 3.9325 mL | 7.8650 mL | |
| 10 mM | 0.3933 mL | 1.9663 mL | 3.9325 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
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