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| Targets |
Furaprofen inhibits HCV replication through a mechanism involving the inhibition of cyclooxygenase (COX), which plays a role in the biosynthesis of pro-inflammatory prostaglandins. By blocking COX activity, furaprofen reduces the formation of pro-inflammatory signaling molecules, thereby alleviating inflammation and pain. The compound also exhibits antidiabetic and antiglycative properties. Furaprofen's anti-HCV activity is substantially more potent against genotype 1a and 1b replicons than against genotype 2a.
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| ln Vitro |
Effective and very specific against HCV replication is furoprofen (R803). Furaprofen's antiviral activity was found to be 29.88±8.05 nM by repeated reporter replicon tests, about three times higher than that of the parent drug R706. The potency of furoprofen against replicons was also validated by TaqMan RT-PCR and Western blotting, coming in at about 37 nM and 54.67±4.11 nM, respectively. A panel of primary cells and transformed human cell lines were treated with increasing dosages of furaprofen for 48 hours in order to evaluate the drug's overall effect on cell proliferation. The impact of the treatment on cell proliferation was determined using an MTS-based cell viability test. Research indicates that furaprofen, at concentrations ranging from 2 μM to ≥10 μM, depending on cell type and proliferative status, causes a 50% reduction in cell counts in the absence of viral infection (CC50) [1].
In vitro, furaprofen is a potent inhibitor of HCV replication with an EC₅₀ of approximately 30 nM for genotype 1a and 1b replicons. The compound is substantially less potent against genotype 2a replicons with an EC₅₀ of approximately 1000 nM. Furaprofen also demonstrates anti-inflammatory activity in cell-based assays, consistent with its COX inhibitory mechanism. The compound's antidiabetic and antiglycative properties have been characterized in additional in vitro studies. |
| ln Vivo |
In vivo, furaprofen inhibits carrageenan-induced paw edema in rats, demonstrating anti-inflammatory activity. At higher doses, the compound inhibits cotton pellet-induced granulomas in rats. As an orally available agent, furaprofen achieves systemic exposure sufficient for both anti-inflammatory and anti-HCV activity. The compound's dual mechanism of action makes it a unique tool for studying HCV infection and inflammation.
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| Enzyme Assay |
Non-cellular enzyme assays for furaprofen involve assessing its inhibition of COX-1 and COX-2 using purified enzyme preparations. The enzyme activity is measured by monitoring the conversion of arachidonic acid to prostaglandins using a spectrophotometric or radiometric assay. IC₅₀ values for COX-1 and COX-2 inhibition are determined from dose-response curves. Anti-HCV activity can be assessed using cell-free HCV replicase assays measuring RNA-dependent RNA polymerase activity.
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| Cell Assay |
In vitro cellular assays for furaprofen involve treating HCV replicon-containing cell lines with the compound and measuring viral RNA replication. Cells harboring subgenomic HCV replicons (genotype 1a, 1b, or 2a) are treated with varying concentrations of furaprofen (1-10,000 nM) for 48-72 hours. Viral RNA levels are quantified by real-time RT-PCR or by measuring a reporter gene (e.g., luciferase) encoded by the replicon. EC₅₀ values for inhibition of replication are determined from dose-response curves.
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| Animal Protocol |
In vivo animal experiments with furaprofen are conducted in rodent models of inflammation and pain. In the carrageenan-induced paw edema model, rats are treated with furaprofen orally or intraperitoneally, and paw swelling is measured at multiple time points post-carrageenan injection. In the cotton pellet granuloma model, rats are implanted with cotton pellets and treated with furaprofen, and granuloma formation is assessed by dry weight of the pellets. Anti-HCV efficacy is assessed in HCV mouse models.
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| ADME/Pharmacokinetics |
Furaprofen has a molecular weight of 282.29 and a molecular formula of C₁₇H₁₄O₃. It is a solid at room temperature with a purity of ≥95%. The compound is soluble in DMSO and other organic solvents. It is typically stored at -20°C, protected from light and moisture. Furaprofen is orally bioavailable with favorable pharmacokinetic properties for systemic administration.
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| Toxicity/Toxicokinetics |
Furaprofen is a research compound for laboratory use only and is not approved for human therapeutic use. In preclinical studies, it has been generally well-tolerated at therapeutic doses. As a COX inhibitor, it may have effects on gastrointestinal and renal function similar to other NSAIDs. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation.
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| References | |
| Additional Infomation |
Drug Indication
This drug has been studied for the treatment of hepatitis (viral, hepatitis C). Furaprofen (R803; CAS 67700-30-5) is an orally available, selective HCV inhibitor with anti-inflammatory activity. It inhibits HCV replication with EC₅₀ of ~30 nM for genotype 1a and 1b replicons. Furaprofen inhibits carrageenan-induced paw edema and cotton pellet-induced granulomas in rats. The compound exhibits antidiabetic and antiglycative properties. It is available from various commercial suppliers for research applications. |
| Molecular Formula |
C17H14O3
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|---|---|
| Molecular Weight |
266.3
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| Exact Mass |
266.094
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| CAS # |
67700-30-5
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| PubChem CID |
37801
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| Appearance |
White to light yellow solid powder
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| Density |
1.23g/cm3
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| Boiling Point |
449.4ºC at 760 mmHg
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| Flash Point |
225.6ºC
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| Index of Refraction |
1.627
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| LogP |
4.287
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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 |
3
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| Heavy Atom Count |
20
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| Complexity |
348
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ODZUWQAFWMLWCF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H14O3/c1-11(17(18)19)13-8-5-9-14-15(10-20-16(13)14)12-6-3-2-4-7-12/h2-11H,1H3,(H,18,19)
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| Chemical Name |
2-(3-phenyl-1-benzofuran-7-yl)propanoic acid
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| Synonyms |
R 803; R-803; Furaprofen
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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 : ~250 mg/mL (~938.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.81 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 (7.81 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 (7.81 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 | 3.7552 mL | 18.7758 mL | 37.5516 mL | |
| 5 mM | 0.7510 mL | 3.7552 mL | 7.5103 mL | |
| 10 mM | 0.3755 mL | 1.8776 mL | 3.7552 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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