| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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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].
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| 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].
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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. |
| References |
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| Additional Infomation |
Loxoprofen sodium is an organic sodium salt having loxoprofen(1-) as the counterion. The parent acid, loxoprofen, is a prodrug that is rapidly converted to its active trans-alcohol metabolite following oral administration. It has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, an EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor and an antipyretic. It contains a loxoprofen(1-).
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| 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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