| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Loxoprofen targets cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2, with IC50s of 6.5 and 13.5 µM, respectively. By inhibiting COX enzymes, it reduces the production of prostaglandins, which are key mediators of inflammation, pain, and fever. It is converted in vivo to the corresponding trans-hydroxycyclopentane analog, through which it appears to exert its activity.
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| ln Vitro |
Loxoprofen sodium is a non-selective COX inhibitor and an anti-inflammatory prodrug (NSAID). The IC50 values for COX-1 and COX-2 in the human whole blood assay are 6.5 and 13.5μM, respectively. [1]. A common non-selective cyclooxygenase inhibitor used to investigate pain and inflammation in both chronic and acute illnesses is loxoprofen (LOX) sodium. Carbonyl reductase (CR) creates its alcohol metabolite, which is made up of both active trans-LOX and inactive cis-LOX. Furthermore, cytochrome P450 (CYP) has the ability to transform LOX sodium into inactive hydroxylated metabolites (OH-LOXs) [2].
In vitro, loxoprofen is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 µM for COX-1 and COX-2, respectively. Its activity is assessed using enzyme assays with purified COX enzymes, measuring the inhibition of prostaglandin production. It has anti-inflammatory, analgesic, and antipyretic properties. It can also reduce atherosclerosis and shows antitumor activity. |
| ln Vivo |
Loxoprofen sodium (4 mg/kg/day; PO; 1 or 8 weeks) lowers atherosclerosis in rats via decreasing inflammation [3]. Loxoprofen sodium (60 μg/mL; oral; 24 days) reduces tumor growth in mice via blocking VEGF [4].
In vivo, loxoprofen is an orally active anti-inflammatory, analgesic, and antipyretic agent. It is used for the management of rheumatoid arthritis and related disorders. It is available in some countries for oral administration. Its activity is mediated through its conversion to an active metabolite. |
| Enzyme Assay |
The in vitro enzyme assay for loxoprofen measures its ability to inhibit cyclooxygenase (COX) activity. These cell-free assays use purified COX-1 and COX-2 enzymes and measure the production of prostaglandins from arachidonic acid. The compound's inhibitory potency (IC50) is determined by measuring the reduction in enzyme activity.
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| Cell Assay |
In vitro cellular assays for loxoprofen assess its anti-inflammatory effects. Cells such as macrophages are treated with loxoprofen, and the production of prostaglandins and other inflammatory mediators is measured. Its effects on cell viability and proliferation can also be assessed.
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| Animal Protocol |
Animal/Disease Models: ApoE-/- mice (C57BL/6J-Apoetm1Unc), 8 to 16 weeks old, high-fat diet (0.2% cholesterol, 21% saturated fat) [3]
Doses: 4 mg/kg/day, given in drinking water Medication method: Oral administration at 8 to 16 weeks of age or 15 to 16 weeks of age. Experimental Results: Inhibition of platelet thromboxane production and platelet aggregation. Reduce the extent of atherosclerosis. Inhibits the production of PGE2, TxB2 and PGI2. Animal/Disease Models: 6weeks old male C57BL/6 and BDF1 mice, 100 μL suspension of LLC cells and KLN205 cells (2×106 cells/mL) were subcutaneously (sc) (sc) injected into C57BL/6 and BDF1 mice respectively [4]. Doses: 60 μg/mL Route of Administration: Orally administered daily for 24 days Experimental Results: Inhibited tumor growth and angiogenesis in LLC tumor mice, inhibited VEGF expression, and inhibited HUVEC tube formation. In vivo animal studies for loxoprofen have been conducted in animal models of inflammation and pain to evaluate its efficacy. However, its clinical efficacy has been established in human use for rheumatoid arthritis and related disorders. |
| ADME/Pharmacokinetics |
Loxoprofen is orally active. It is absorbed from the gastrointestinal tract and distributed throughout the body. It is converted in vivo to its active metabolite. Its pharmacokinetic properties support its use as an oral NSAID.
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| Toxicity/Toxicokinetics |
Loxoprofen is generally well-tolerated. Common adverse effects include gastrointestinal disturbances, which are typical of NSAIDs. It should be used with caution in patients with a history of peptic ulcer disease or renal impairment. Its safety profile has been established through clinical use.
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| References |
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| Additional Infomation |
Loxoprofen sodium is an organic sodium salt with the counterion loxoprofen(1-). The parent acid loxoprofen is a prodrug that is rapidly converted to its active trans-alcohol metabolite after oral administration. It has the effects of a nonsteroidal anti-inflammatory drug, a non-narcotic analgesic, an EC 1.14.99.1 (prostaglandin intraperoxidase) inhibitor, and an antipyretic. It contains the loxoprofen(1-) ion.
Loxoprofen (CAS 80382-23-6) is a non-steroidal, orally active anti-inflammatory agent with analgesic and antipyretic properties. It is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 µM for COX-1 and COX-2, respectively. It has a molecular formula of C15H17NaO3 and a molecular weight of 268.28. It is available as a prescription medication in some countries. |
| Molecular Formula |
C15H17NAO3
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| Molecular Weight |
268.2835
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| Exact Mass |
268.107
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| CAS # |
80382-23-6
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| Related CAS # |
Loxoprofen;68767-14-6;Loxoprofen sodium (dihydrate);226721-96-6
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| PubChem CID |
23663407
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| Appearance |
White to off-white solid powder
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| Boiling Point |
417.9ºCat 760 mmHg
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| Flash Point |
220.7ºC
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| LogP |
1.451
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
321
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WORCCYVLMMTGFR-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C15H18O3.Na/c1-10(15(17)18)12-7-5-11(6-8-12)9-13-3-2-4-14(13)16;/h5-8,10,13H,2-4,9H2,1H3,(H,17,18);/q;+1/p-1
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| Chemical Name |
sodium;2-[4-[(2-oxocyclopentyl)methyl]phenyl]propanoate
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O : ~100 mg/mL (~372.74 mM)
DMSO : ~19.23 mg/mL (~71.68 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.92 mg/mL (7.16 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 19.2 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: ≥ 1.92 mg/mL (7.16 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 19.2 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: ≥ 1.92 mg/mL (7.16 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 | 3.7274 mL | 18.6372 mL | 37.2745 mL | |
| 5 mM | 0.7455 mL | 3.7274 mL | 7.4549 mL | |
| 10 mM | 0.3727 mL | 1.8637 mL | 3.7274 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 |
| NCT03800797 | Completed | Drug: Loxoprofen sodium hydrogel patch
Drug: Loxoprofen sodium tablet |
Ankylosing Spondylitis | Sun Yat-sen University | 2015-05-25 | Phase 4 |
| NCT06510413 | Not yet recruiting | Drug: Loxoprofen Sodium Patches(reference product) Drug: Loxoprofen Sodium Patches(test product ) |
Muscle Pain Osteoarthritis Swelling Muscle |
Frontier Biotechnologies Inc. | 2024-07 | Phase 1 |
| NCT01779271 | Completed | Drug: Pelubiprofen Drug: Loxoprofen |
Acute Upper Respiratory Infection Fever |
Daewon Pharmaceutical Co., Ltd. | 2013-01 | Phase 3 |
| NCT00676117 | Completed | Drug: Esomeprazole (D961H) Drug: Loxoprofen |
Healthy | AstraZeneca | 2008-04 | Phase 1 |
| NCT04386122 | Completed | Drug: FABALOFEN 60 Drug: JAPROLOX TABLET |
Bioequivalence | Centre of Clinical Pharmacology, Hanoi Medical University | 2020-05-07 | Phase 1 |
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