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Purity: ≥98%
Mofezolac (formerly known as N-22; trade name in Japan: Disopain) is a highly selective COX-1 (cyclooxygenase-1) inhibitor with COXs selectivity index > 6000. It is a nonsteroidal anti-inflammatory drug (NSAID) used as an analgesic and anti-inflammatory drug for the treatment of rheumatoid arthritis, lower back pain, frozen shoulder, and pain management after surgery or trauma. Mofezolac has the potential to treat pain, musculoskeletal pain, and arthritis. Prostaglandin endoperoxide synthases or cyclooxygenases (COX-1 and COX-2), which play a critical role in the inflammation, are the pharmacological targets of non-steroidal anti-inflammatory drugs, used to treat pain and inflammation. The capability of P6 and mofezolac to modulate the NF-kB signaling pathway, emphasizing the neuroprotective effect and therapeutic potential of COX-1 inhibitors in the control of neuroinflammatory diseases.
| ln Vitro |
Using the human platelet-rich plasma (hPRP) assay, mofezolac inhibits platelet aggregation with an IC50 of 0.45 μM [2]. When administered in conjunction with the proteasome inhibitor Bortezomib, mofezolac modifies the MM cell cycle and apoptosis and marginally amplifies the cytotoxic effect of Bortezomib on the multiple myeloma (MM) cell lines (NCI-H929 and RPMI-8226) [2].
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| ln Vivo |
Mice injected intraperitoneally with phenyl-p-benzoquinone do not writhe when given murfezolic acid (1–30 mg/kg; oral; once) [1].
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| Animal Protocol |
Animal/Disease Models: Female ddY mice (4 weeks old, 18-27 g) were injected with phenyl-p-benzoquinone (PQ) [1]
Doses: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Route of Administration: Oral; Experimental Results:Dose-dependent inhibition of writhing in mice induced by PQ injection. |
| References |
[1]. K Goto, et al. Analgesic effect of mofezolac, a non-steroidal anti-inflammatory drug, against phenylquinone-induced acute pain in mice. Prostaglandins Other Lipid Mediat. 1998 Jul;56(4):245-54.
[2]. Maria Laura Pati, et al. Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability. Eur J Med Chem. 2019 Feb 15;164:59-76. |
| Molecular Formula |
C19H17NO5
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| Molecular Weight |
339.35
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| CAS # |
78967-07-4
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| Related CAS # |
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| SMILES |
O=C(O)CC1=C(C2=CC=C(OC)C=C2)C(C3=CC=C(OC)C=C3)=NO1
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| Chemical Name |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.37 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 (7.37 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 (7.37 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 | 2.9468 mL | 14.7341 mL | 29.4681 mL | |
| 5 mM | 0.5894 mL | 2.9468 mL | 5.8936 mL | |
| 10 mM | 0.2947 mL | 1.4734 mL | 2.9468 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.
 Chemical structure of P6 andmofezolac. IC50values refer to the human whole blood assay.Front Neurol.2017 Jun 9;8:251. |
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 Effect ofmofezolacon glial fibrillary acidic protein (GFAP), ionized calcium-binding adapter molecule-1 (Iba-1), cyclooxygenases (COXs), and pIkBα expression in(A)caudate–putamen,(B)hippocampus,(C)frontal lobe, and(D)substantia nigra from mice treated with lipopolysaccharide (LPS) alone and LPS in the presence ofmofezolac.Front Neurol.2017 Jun 9;8:251. |
 Effects of cyclooxygenase (COX)-1 inhibitors on the COXs expression and NF-kB phosphorylation induced by lipopolysaccharide (LPS) in BV2 microglial cells.Front Neurol.2017 Jun 9;8:251. |
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