| Size | Price | Stock | Qty |
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| 100mg |
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| Other Sizes |
| Targets |
Tolmetin sodium dihydrate targets cyclooxygenase (COX-1 and COX-2). It is a potent COX inhibitor with IC50s of 0.35 µM for human COX-1 and 0.82 µM for human COX-2. By inhibiting COX enzymes, the compound reduces the conversion of arachidonic acid into prostaglandins and thromboxanes that mediate inflammation and pain. The compound also inhibits aldo-keto reductases and acts as a beta-adrenergic blocker.
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| ln Vitro |
Rat brain homogenates show no reduction in lipid peroxidation when tolmetin sodium dihydrate (0.25 mM) is added. In rat brain homogenate, tolmetin (0.25, 0.5, 0.75, and 1 mM) demonstrates free radical scavenging activities without producing superoxide anion [3]. The HT-29 colon cancer cell line is susceptible to dose-dependent anticancer action from tolmetin sodium dihydrate (0.001-100 μM) [4]. On osteoblast development, tolmetin sodium dihydrate (0-100 μM) has little effect [5].
In vitro, Tolmetin sodium dihydrate inhibits COX-1 and COX-2 with IC50s of 0.35 µM and 0.82 µM, respectively. It inhibits aldo-keto reductases (e.g., IC50 = 2.39 µM for human aldose reductase). The compound's in vitro activity is well-characterized and forms the basis for its use as an NSAID. |
| ln Vivo |
Maximum ulcerogenic effects were observed 4 hours after a single dose of tolmetin sodium dihydrate (30,100 mg/kg; gavage; once or twice daily for 3 and 14 days). In male Wistar rats weighing 180 g, the ulcerogenic effect of -200 g was significantly reduced after repeated administration for 3 and 14 days. At 100 mg/kg, tolmetin can induce stomach injury [2]. Quinolinic acid (QA)-induced neurotoxicity was considerably reduced when tolmetin sodium dihydrate (5 mg/kg twice day for 5 days) was administered beforehand [3].
In vivo, Tolmetin sodium dihydrate is an orally active NSAID used for its analgesic, anti-inflammatory, and antipyretic effects. It is used for the symptomatic treatment of osteoarthritis and rheumatoid arthritis. It is also used for the management of juvenile rheumatoid arthritis and ankylosing spondylitis. The compound's in vivo efficacy is attributed to its COX inhibition. |
| Enzyme Assay |
Cell-free COX enzyme assays with Tolmetin sodium dihydrate are performed using purified COX-1 or COX-2 enzymes. The enzyme is incubated with arachidonic acid substrate and varying concentrations of Tolmetin. Prostaglandin production is measured by ELISA or radioimmunoassay to determine IC50 values. These cell-free assays are essential for characterizing the potency of Tolmetin sodium dihydrate as a COX inhibitor.
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| Cell Assay |
In cellular assays, inflammatory cell lines or primary cells are treated with Tolmetin sodium dihydrate. Prostaglandin E2 production is measured by ELISA. Inflammatory cytokine production and NF-κB activation are assessed. Cell viability is evaluated to determine cytotoxicity. These cellular assays are crucial for understanding the functional consequences of COX inhibition and for validating the compound's activity as an NSAID.
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| Animal Protocol |
Tolmetin sodium dihydrate is evaluated in animal models of inflammation (e.g., carrageenan-induced paw edema) and pain (e.g., writhing test). The compound is administered orally. Edema reduction, pain relief, and fever reduction are assessed. These in vivo studies are essential for confirming the compound's efficacy in a physiologically relevant context.
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| ADME/Pharmacokinetics |
Tolmetin sodium dihydrate is orally bioavailable. Following oral administration, it is absorbed from the gastrointestinal tract and distributed to tissues. Pharmacokinetic parameters including Cmax, Tmax, and half-life have been characterized.
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| Toxicity/Toxicokinetics |
NSAIDs including Tolmetin may cause gastrointestinal irritation, ulceration, and renal effects. Standard toxicology studies in animals evaluate gastrointestinal, renal, and hepatic toxicity. The compound is contraindicated in patients with NSAID hypersensitivity.
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| References |
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| Additional Infomation |
Tometrin sodium dihydrate is an organosodium salt, the dihydrate form of Tometrin sodium. It is a nonselective nonsteroidal anti-inflammatory drug (NSAID). It is an EC 1.14.99.1 (prostaglandin intraperoxidase) inhibitor, and also an NSAID. It is an organosodium salt and hydrate. It contains Tometrin sodium.
See also: Tometrin sodium (note moved to). Tolmetin sodium dihydrate (CAS 64490-92-2) is an FDA-approved NSAID. It is available as a pharmaceutical product for the treatment of pain and inflammation. The compound is also used in dermatological research to study skin inflammation and barrier stress pathways. It is available as a research-grade reference compound. When handling Tolmetin sodium dihydrate, researchers should follow standard safety protocols for handling chemical reagents, including the use of appropriate personal protective equipment and working in a well-ventilated area. |
| Molecular Formula |
C15H14NO3-.NA+.2[H2O]
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|---|---|
| Molecular Weight |
315.29692
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| Exact Mass |
315.108
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| CAS # |
64490-92-2
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| Related CAS # |
Tolmetin;26171-23-3;Tolmetin sodium;35711-34-3
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| PubChem CID |
23677829
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
483.2ºC at 760 mmHg
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| Melting Point |
155-157 (dec.)
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| Flash Point |
246ºC
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| LogP |
0.728
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
353
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QQILXENAYPUNEA-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C15H15NO3.Na.2H2O/c1-10-3-5-11(6-4-10)15(19)13-8-7-12(16(13)2)9-14(17)18;;;/h3-8H,9H2,1-2H3,(H,17,18);;2*1H2/q;+1;;/p-1
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| Chemical Name |
sodium;2-[1-methyl-5-(4-methylbenzoyl)pyrrol-2-yl]acetate;dihydrate
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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, 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 (~317.16 mM)
DMSO : ~12.5 mg/mL (~39.64 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.96 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 12.5 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: ≥ 1.25 mg/mL (3.96 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 12.5 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: ≥ 1.25 mg/mL (3.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (79.29 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1716 mL | 15.8579 mL | 31.7158 mL | |
| 5 mM | 0.6343 mL | 3.1716 mL | 6.3432 mL | |
| 10 mM | 0.3172 mL | 1.5858 mL | 3.1716 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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