| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Targets |
Pelubiprofen targets the cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2. By inhibiting these enzymes, it blocks the conversion of arachidonic acid to prostaglandin H2, the precursor of various prostaglandins and thromboxanes. This results in reduced production of prostaglandins involved in inflammation, pain, and fever. Pelubiprofen exhibits anti-inflammatory, analgesic, and antipyretic effects through this mechanism of action.
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| ln Vitro |
In vitro, Pelubiprofen has been shown to inhibit COX-1 and COX-2 enzyme activity in a concentration-dependent manner. It effectively reduces the production of prostaglandin E2 (PGE2) in various cell types. Pelubiprofen also demonstrates antioxidant properties in some in vitro assays. Studies have investigated its effects on various inflammatory mediators and signaling pathways, including NF-κB and MAPK pathways, which contribute to its anti-inflammatory effects.
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| ln Vivo |
In vivo, Pelubiprofen has been shown to produce dose-dependent anti-inflammatory, analgesic, and antipyretic effects in animal models. It is effective in reducing carrageenan-induced paw edema, a standard model of acute inflammation. Pelubiprofen has also been shown to be effective in chronic inflammatory models, such as adjuvant-induced arthritis. Clinical studies have demonstrated its efficacy in reducing pain and inflammation in patients with rheumatoid arthritis, osteoarthritis, and other inflammatory conditions.
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| Enzyme Assay |
In vitro enzyme inhibition assays for Pelubiprofen typically involve measuring the activity of COX-1 and COX-2 enzymes in the presence of varying concentrations of the compound. The enzymes are incubated with arachidonic acid substrate, and the production of prostaglandins is measured using ELISA, radioimmunoassay, or other detection methods. The IC50 values for COX-1 and COX-2 inhibition are determined from dose-response curves. The compound is typically dissolved in DMSO and diluted in assay buffer.
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| Cell Assay |
In vitro cell-based studies with Pelubiprofen typically involve cultured inflammatory cells such as macrophages or synoviocytes. Cells are treated with Pelubiprofen at various concentrations in the presence or absence of inflammatory stimuli such as lipopolysaccharide (LPS) or cytokines. The production of inflammatory mediators such as PGE2, TNF-α, IL-1β, and IL-6 is measured by ELISA. The effect of Pelubiprofen on cell viability and proliferation can be assessed using MTT or similar assays.
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| Animal Protocol |
In vivo animal studies with Pelubiprofen are typically conducted in rodent models to evaluate its anti-inflammatory, analgesic, and antipyretic efficacy. The compound is administered orally or intraperitoneally. The anti-inflammatory effect is assessed using the carrageenan-induced paw edema model or the adjuvant-induced arthritis model. Analgesic activity is evaluated using the tail-flick test, hot-plate test, or writhing test. Antipyretic activity is assessed in yeast-induced fever models. Pharmacokinetic studies are performed by measuring Pelubiprofen concentrations in plasma and tissues.
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| ADME/Pharmacokinetics |
Pelubiprofen is a well-characterized drug with established pharmacokinetic properties. Following oral administration, it is rapidly absorbed from the gastrointestinal tract. Pelubiprofen is highly protein-bound (approximately 99%) to plasma proteins. It is extensively metabolized in the liver, primarily by cytochrome P450 enzymes, to inactive metabolites. The elimination half-life is approximately 2-4 hours. Pelubiprofen is excreted in the urine primarily as metabolites. The pharmacokinetic profile of Pelubiprofen is similar to that of other propionic acid NSAIDs.
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| Toxicity/Toxicokinetics |
Pelubiprofen is a clinically approved NSAID with a well-established safety profile. The most common adverse effects are gastrointestinal, including dyspepsia, nausea, abdominal pain, and diarrhea. As with other NSAIDs, Pelubiprofen can cause gastrointestinal bleeding, ulceration, and perforation, particularly with long-term use. Cardiovascular effects such as increased blood pressure and risk of thrombotic events have been reported. Renal effects, including fluid retention and decreased renal function, can occur. Allergic reactions are rare.
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| Additional Infomation |
The use of peribirofen for the treatment of chronic back pain has been studied.
Pelubiprofen is a clinically approved NSAID used for the treatment of inflammatory conditions such as rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, and acute pain. It is available in various formulations, including tablets and capsules. Pelubiprofen is structurally related to ibuprofen and shares a similar pharmacological profile. It is generally well-tolerated, with a safety profile similar to other propionic acid NSAIDs. The compound is available in several countries under various brand names. |
| Molecular Formula |
C16H18O3
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|---|---|
| Molecular Weight |
258.31232
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| Exact Mass |
258.125
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| CAS # |
69956-77-0
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| Related CAS # |
Pelubiprofen-13C,d3
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| PubChem CID |
5282203
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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 |
457.4±34.0 °C at 760 mmHg
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| Flash Point |
244.5±22.2 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.605
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| LogP |
2.76
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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 |
19
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| Complexity |
376
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C1=CC=C(C=C1)/C=C/2\CCCCC2=O)C(=O)O
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| InChi Key |
AUZUGWXLBGZUPP-GXDHUFHOSA-N
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| InChi Code |
InChI=1S/C16H18O3/c1-11(16(18)19)13-8-6-12(7-9-13)10-14-4-2-3-5-15(14)17/h6-11H,2-5H2,1H3,(H,18,19)/b14-10+
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| Chemical Name |
2-[4-[(E)-(2-oxocyclohexylidene)methyl]phenyl]propanoic 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 (~387.13 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.68 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 25.0 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: ≥ 2.5 mg/mL (9.68 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 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.68 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 | 3.8713 mL | 19.3566 mL | 38.7132 mL | |
| 5 mM | 0.7743 mL | 3.8713 mL | 7.7426 mL | |
| 10 mM | 0.3871 mL | 1.9357 mL | 3.8713 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01870102 | Completed | Drug: Pelubiprofen IR (Pelubiprofen 30mg) TID
Drug: Pelubiprofen SR (Pelubiprofen 45 mg) BID |
Healthy Males | Daewon Pharmaceutical Co., Ltd. | Phase 1 | |
| NCT01776697 | Completed | Drug: pelubiprofen (30mg) tablet IR Drug: pelubiprofen SR (as a pelubiprofen 90 mg) tablet |
Healthy | Daewon Pharmaceutical Co., Ltd. | 2012-03 | Phase 1 |
| NCT03874247 | Unknown status | Drug: pelubiprofen 45mg Drug: pelubiprofen placebo |
Acute Traumatic Injury | Daewon Pharmaceutical Co., Ltd. | 2019-02-25 | Phase 3 |
| NCT01779271 | Completed | Drug: Pelubiprofen Drug: Loxoprofen |
Acute Upper Respiratory Infection Fever |
Daewon Pharmaceutical Co., Ltd. | 2013-01 | Phase 3 |
| NCT02375633 | Completed | Drug: DW-330SR2 Drug: Pelubiprofen |
Chronic Back Pain | Daewon Pharmaceutical Co., Ltd. | 2014-04 | Phase 3 |
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