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| 5mg |
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| Targets |
Furobufen targets cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2. By inhibiting these enzymes, it reduces the production of prostaglandins, which are mediators of inflammation, pain, and fever. The compound is a prodrug that is metabolized to its active metabolite, which is responsible for its COX-inhibiting activity. Its mechanism of action is characteristic of the NSAID class of drugs.
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| ln Vitro |
In vitro, furobufen exhibits anti-inflammatory activity by inhibiting COX enzymes and reducing prostaglandin production. Its activity has been demonstrated in various in vitro assays measuring prostaglandin synthesis. The compound's ability to inhibit COX-1 and COX-2 has been characterized. Its analgesic and anti-inflammatory effects have been observed in cell-based models.
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| ln Vivo |
In male rats weighing 180-200 g, furbufen (oral; 10, 30, 90 mg/kg; once daily; 7 days) causes a dose-related inhibitory effect on carrageenan-induced paw edema [1].
In vivo, furobufen has demonstrated analgesic and anti-inflammatory effects in animal models. It was studied for the treatment of rheumatoid arthritis and osteoarthritis. The compound's efficacy in reducing inflammation and pain has been evaluated in preclinical studies. Its development was discontinued, and it is not currently marketed for clinical use. |
| Enzyme Assay |
In vitro enzyme assays for furobufen involve measuring the inhibition of COX-1 and COX-2 activity using purified enzyme preparations. The compound is first converted to its active metabolite, and then incubated with COX enzymes and arachidonic acid. Prostaglandin production is measured using immunoassays or other detection methods. The IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for furobufen involve treating cells with the compound to assess its effects on prostaglandin production and inflammation. Cells are stimulated with inflammatory mediators, and prostaglandin levels are measured by ELISA. The compound's effects on cell viability and inflammatory markers are also assessed. These assays characterize its anti-inflammatory activity.
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| Animal Protocol |
In vivo animal experiments for furobufen have been conducted in models of inflammation and pain. The compound is typically administered orally. Efficacy endpoints include reduction in paw edema in carrageenan-induced inflammation models and reduction in pain responses in various pain models. Its effects on inflammatory markers are also assessed.
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| ADME/Pharmacokinetics |
Furobufen has a molecular weight and formula consistent with butyric acid derivatives. It is a prodrug that is metabolized to its active form in the body. The compound is typically dissolved in DMSO for in vitro studies and formulated for oral administration in vivo. Its pharmacokinetic properties, including absorption, distribution, metabolism, and elimination, have been characterized in preclinical studies.
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| Toxicity/Toxicokinetics |
Specific toxicity data for furobufen is not extensively reported. As an NSAID, its safety profile is likely similar to other drugs in this class, which can cause gastrointestinal, renal, and cardiovascular side effects. The compound's development was discontinued, possibly due to safety or efficacy concerns. Standard safety precautions should be taken when handling the compound.
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| References |
[1]. Martel RR, et al. Anti-inflammatory properties of furobufen. Can J Physiol Pharmacol. 1974 Jun;52(3):669-73.
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| Additional Infomation |
Furobufen is a nonsteroidal anti-inflammatory drug (NSAID) and a butyric acid derivative. It is a prodrug that was studied for the treatment of rheumatoid arthritis and osteoarthritis. The compound's development was discontinued, and it is not currently marketed. Furobufen is a research compound used in anti-inflammatory research.
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| Molecular Formula |
C16H12O4
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|---|---|
| Molecular Weight |
268.26408
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| Exact Mass |
268.074
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| CAS # |
38873-55-1
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| PubChem CID |
38117
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.343g/cm3
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| Boiling Point |
509.8ºC at 760 mmHg
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| Flash Point |
262.1ºC
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| Index of Refraction |
1.676
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| LogP |
3.633
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
392
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(CCC(c1cc(c2ccccc2o3)c3cc1)=O)=O
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| InChi Key |
LQVMQEYROPXMQH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12O4/c17-13(6-8-16(18)19)10-5-7-15-12(9-10)11-3-1-2-4-14(11)20-15/h1-5,7,9H,6,8H2,(H,18,19)
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| Chemical Name |
4-dibenzofuran-2-yl-4-oxobutanoic acid
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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 : ~100 mg/mL (~372.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7277 mL | 18.6386 mL | 37.2773 mL | |
| 5 mM | 0.7455 mL | 3.7277 mL | 7.4555 mL | |
| 10 mM | 0.3728 mL | 1.8639 mL | 3.7277 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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