Meclofenamate Sodium (Meclonax; Meclomen; INF-4668; INF4668; CI 583; CI-583; Meclodium; Meclofenamic acid sodium) is a potent nonsteroidal anti-inflammatory drug (NSAID), acting as a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM, respectively. It is used in the treatment of joint, muscular pain, arthritis and dysmenorrhea. Meclofenamate sodium is a potent nonsteroidal antiinflammatory agent, specifically inhibits chemotactic factor-induced human polymorphonuclear leukocyte functions: chemotaxis, degranulation, and generation of superoxide anion radicals. These effects of MSM were found to be dependent upon the concentrations of drug not bound to albumin (free drug), and were caused by its ability to interfere at both a receptor and post-receptor level.
Physicochemical Properties
| Molecular Formula | C14H11CL2NO2.NA | |
| Molecular Weight | 318.13 | |
| Exact Mass | 335.009 | |
| CAS # | 6385-02-0 | |
| Related CAS # | Meclofenamic acid;644-62-2 | |
| PubChem CID | 4038 | |
| Appearance | White to off-white solid powder | |
| Boiling Point | 399.4ºC at 760 mmHg | |
| Melting Point | 287 °C | |
| Flash Point | 195.3ºC | |
| LogP | 3.481 | |
| Hydrogen Bond Donor Count | 1 | |
| Hydrogen Bond Acceptor Count | 3 | |
| Rotatable Bond Count | 3 | |
| Heavy Atom Count | 20 | |
| Complexity | 332 | |
| Defined Atom Stereocenter Count | 0 | |
| InChi Key | QHJLLDJTVQAFAN-UHFFFAOYSA-M | |
| InChi Code | InChI=1S/C14H11Cl2NO2.Na.H2O/c1-8-6-7-10(15)13(12(8)16)17-11-5-3-2-4-9(11)14(18)19;;/h2-7,17H,1H3,(H,18,19);;1H2/q;+1;/p-1 | |
| Chemical Name | sodium 2-((2,6-dichloro-3-methylphenyl)amino)benzoate hydrate | |
| Synonyms |
|
|
| HS Tariff Code | 2934.99.9001 | |
| 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 and light. |
|
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation ◉ Summary of Use during Lactation Because no information is available on the use of meclofenamate during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References | J Mol Cell Cardiol.2016May;94:131-44; |
| Additional Infomation |
Sodium meclofenamate (anhydrous) is an organic sodium salt. It contains a meclofenamic acid(1-). A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis. See also: Meclofenamate Sodium (annotation moved to). |
Solubility Data
| Solubility (In Vitro) |
|
|||
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.54 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 (6.54 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. Solubility in Formulation 3: ≥ 2.08 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1434 mL | 15.7168 mL | 31.4337 mL | |
| 5 mM | 0.6287 mL | 3.1434 mL | 6.2867 mL | |
| 10 mM | 0.3143 mL | 1.5717 mL | 3.1434 mL |