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| 1mg |
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| 5mg |
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| Other Sizes |
Meclofenamic Acid (INF-4668; CI 583; INF4668; CI-583; Meclonax; Meclomen; Meclodium) is a potent anti-inflammatory agent of the NSAID (nonsteroidal anti-inflammatory drug) class. It acts as a dual COX-1/COX-2 inhibitor with IC50s of 40 nM and 50 nM, respectively. Meclofenamic Acid has been approved for use in the treatment of joint, muscular pain, arthritis and dysmenorrhea.
| ln Vitro |
Meclofenamic acid inhibits FTO demethylation in a dose-response manner (0-100 μM, 24 hours) [1]. Meclofenamic acid suppresses prostaglandin synthesis by inhibiting cyclooxygenase, having an IC50 of about 1 μM [2]. Meclofenamic acid counteracts tissue reactions to certain prostaglandins and suppresses the production of 5-HETE and LTB4 from human neutrophils when induced by calcium ionophores [2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HeLa Cell Tested Concentrations: 0, 12.5, 25, 50, 100 μM Incubation Duration: 24 h Experimental Results: Inhibited FTO demethylation in a dose-response manner and increased the level of m6A in cellular mRNA Targeting FTO. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Meclofenamic acid is rapidly absorbed by the body after a single or multiple oral dose, with peak plasma concentrations reached within 0.5 to 2 hours. Concomitant use of antacids (aluminum hydroxide and magnesium hydroxide) does not interfere with its absorption. Unlike most nonsteroidal anti-inflammatory drugs (NSAIDs), which show a reduced absorption rate but not necessarily a decrease in the extent of absorption when taken with food, meclofenamic acid exhibits both a reduced absorption rate and an decreased extent of absorption when taken with food. It has been reported that taking meclofenamic acid capsules half an hour after a meal reduces average bioavailability by 26%, decreases average peak concentration (Cmax) by four times, and delays the time to peak concentration by 3 hours. Other metabolites (with unknown excretion rates) comprise 35% to 62% of the remaining dose and are excreted in the urine. The remaining dose (approximately 30%) is excreted in the feces (apparently via bile). Trace amounts of meclofenamic acid sodium are secreted into human breast milk. 9.1 to 43.2 liters Oral clearance = 206 mL/min Metabolism/Metabolites Hepatic metabolism. Meclofenamic acid is extensively metabolized into one active metabolite (metabolite I; the 3-hydroxymethyl metabolite of meclofenamic acid) and at least six other minor metabolites with less well-defined characteristics. In vitro studies have shown that only metabolite I inhibits cyclooxygenase activity, with an activity approximately one-fifth that of meclofenamic acid. Biological half-life A study in 10 healthy subjects showed that the apparent elimination half-life after a single oral dose ranged from 0.8 to 5.3 hours. The mean half-life of metabolite I (the 3-hydroxymethyl metabolite of meclofenamic acid) is approximately 15 hours. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation Since there is currently no information regarding the use of meclofenamic acid during lactation, alternative medications may be preferred, especially for breastfed newborns or premature infants. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. Protein Binding Over a wide range of drug concentrations, the binding rate to plasma proteins is greater than 99%. |
| References |
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| Additional Infomation |
Meclofenamic acid is an aminobenzoic acid, a derivative of anthranilic acid, in which a hydrogen atom bonded to a nitrogen atom is replaced by 2,6-dichloro-3-methylphenyl. It is a nonsteroidal anti-inflammatory drug (NSAID), and its sodium salt is used to treat dysmenorrhea, osteoarthritis, and rheumatoid arthritis. It possesses a variety of pharmacological effects, including NSAID, antirheumatic, antitumor, anticonvulsant, analgesic, antipyretic, EC 1.13.11.34 (arachidonic acid 5-lipoxygenase) inhibitor, and EC 1.14.99.1 (prostaglandin endoperoxidase) inhibitor. It is an aminobenzoic acid, a secondary amino compound, and an organochlorine compound. It is the conjugate acid of meclofenamic acid (1-). It is a NSAID with antipyretic and antigranulomatous effects. It also inhibits prostaglandin biosynthesis. It also inhibits prostaglandin biosynthesis.
See also: Meclofenamic acid sodium (in salt form). IndicationsFor the relief of mild to moderate pain, and for the treatment of primary dysmenorrhea and idiopathic menorrhagia. It can also be used to relieve the signs and symptoms of acute and chronic rheumatoid arthritis and osteoarthritis. Mechanism of Action Like other nonsteroidal anti-inflammatory drugs (NSAIDs), its mechanism of action is not fully understood. Its therapeutic effect does not stem from stimulation of the pituitary-adrenal axis. Animal studies have shown that meclofenamic acid inhibits prostaglandin synthesis and competes with prostaglandin receptors for binding sites. In vitro studies have shown that meclofenamic acid inhibits the activity of human leukocyte 5-lipoxygenase. These properties may explain the anti-inflammatory effect of meclofenamic acid. There is currently no evidence that meclofenamic acid alters the course of the primary disease. Pharmacodynamics Meclofenamic acid is a nonsteroidal anti-inflammatory drug (NSAID) that has been shown to have anti-inflammatory, analgesic, and antipyretic effects in experimental animals. |
| Molecular Formula |
C14H11CL2NO2
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|---|---|
| Molecular Weight |
296.15
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| Exact Mass |
295.016
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| CAS # |
644-62-2
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| Related CAS # |
Meclofenamic acid sodium;6385-02-0;Meclofenamic acid sodium hydrate;67254-91-5;Meclofenamic acid-d4;1185072-18-7;Meclofenamic acid-13C6
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| PubChem CID |
4037
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| Appearance |
White to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
399.4±42.0 °C at 760 mmHg
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| Melting Point |
257-259ºC
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| Flash Point |
195.3±27.9 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.663
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| LogP |
6.67
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| Hydrogen Bond Donor Count |
2
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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 |
327
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SBDNJUWAMKYJOX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H11Cl2NO2/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)
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| Chemical Name |
2-(2,6-dichloro-3-methylanilino)benzoic acid
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| Synonyms |
INF-4668CI 583INF4668 CI-583Meclonax Meclomen Meclodium
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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) |
MEthanol : ~7.14 mg/mL (~24.11 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3767 mL | 16.8833 mL | 33.7667 mL | |
| 5 mM | 0.6753 mL | 3.3767 mL | 6.7533 mL | |
| 10 mM | 0.3377 mL | 1.6883 mL | 3.3767 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.
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