| Size | Price | Stock | Qty |
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| 5g |
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| 10g |
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| Other Sizes |
| Targets |
Cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). Tenoxicam inhibits both COX-1 and COX-2 enzymes, reducing the synthesis of prostaglandins from arachidonic acid. This inhibition accounts for its anti-inflammatory, analgesic, and antipyretic effects. As prostaglandins sensitize pain receptors, their inhibition mediates peripheral analgesic effects. Antipyresis may occur through central action on the hypothalamus.
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| ln Vitro |
One nonsteroidal anti-inflammatory medication (NSAID) is tenoxicam (Ro-12-0068) [1].
Tenoxicam demonstrates anti-inflammatory activity in vitro by inhibiting COX enzyme activity and prostaglandin synthesis. The compound has been characterized in various in vitro assays for its ability to inhibit prostaglandin production. Its potency and selectivity for COX-1 versus COX-2 have been studied. |
| ln Vivo |
Tenoxicam (Ro-12-0068) was administered intraperitoneally immediately after BCAO. Histological investigation demonstrated that ischemia induced considerable striatal and hippocampal damage that was alleviated by treatment with tenoxicam (Ro-12-0068). Tenoxicam (Ro-12-0068) also significantly lowers the elevated myeloperoxidase activity found in hippocampus homogenates following ischemia to control levels [2].
In vivo, Tenoxicam has been shown to reduce kaolin-induced edema in rat hind paw with an ED30 of 2.6 mg/kg and threshold pain response with an ED100 of 5.3 mg/kg. It is used clinically to treat osteoarthritis, rheumatoid arthritis, and acute pain. The drug is administered orally and has a long half-life allowing once-daily dosing. |
| Enzyme Assay |
In vitro enzyme assays for Tenoxicam involve measuring COX-1 and COX-2 activity in the presence of varying concentrations of the compound. The enzymes are incubated with arachidonic acid substrate, and prostaglandin production is measured using ELISA or other detection methods. IC50 values are determined from dose-response curves.
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| Cell Assay |
Cellular assays for Tenoxicam are not typically performed for routine characterization. However, the compound's effects on prostaglandin production can be assessed in cell culture systems such as macrophages or fibroblasts stimulated with LPS or other inflammatory stimuli. Cells are treated with Tenoxicam, and prostaglandin E2 production is measured by ELISA.
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| Animal Protocol |
In vivo animal studies for Tenoxicam have been conducted in rat models of inflammation and pain. The compound is typically administered orally. Anti-inflammatory activity is assessed in the carrageenan-induced paw edema model or kaolin-induced edema model. Analgesic activity is assessed in the acetic acid-induced writhing test or hot plate test. ED30 and ED100 values are determined.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Tenoxicam is rapidly and completely absorbed orally (100% absolute bioavailability). Metabolism/Metabolites Tenoxicam is metabolized in the liver to several less pharmacologically active metabolites (primarily 5'-hydroxytenoxicam). Known metabolites of tenoxicam in humans include 5'-hydroxytenoxicam. Biological Half-Life 72 hours (range 59 to 74 hours) Tenoxicam is well absorbed after oral administration and has a long half-life, allowing once-daily dosing. The drug is highly protein-bound and is metabolized in the liver. It is excreted in urine and bile. The pharmacokinetics of Tenoxicam have been studied in various patient populations, including elderly patients. Its molecular weight is 337.37. |
| Toxicity/Toxicokinetics |
Protein Binding
99% Tenoxicam is generally well-tolerated but can cause gastrointestinal side effects typical of NSAIDs, including gastric irritation and ulceration. It should be used with caution in patients with a history of gastrointestinal bleeding or renal impairment. The drug is approved for clinical use in many countries. Adverse effects may include nausea, dyspepsia, and dizziness. |
| References | |
| Additional Infomation |
Tenoxicam is a thienoxicam monocarboxylic acid amide, formed by the condensation of the carboxyl group of 1,1-dioxide of 4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid with the amino group of 2-aminopyridine. It is used to treat pain and inflammation caused by osteoarthritis and rheumatoid arthritis. It is also indicated for short-term treatment of acute musculoskeletal disorders, including strains, sprains, and other soft tissue injuries. It is a nonsteroidal anti-inflammatory drug, a non-narcotic analgesic, an antipyretic, and also a prostaglandin intraperoxidase (EC 1.14.99.1) inhibitor. It is a heteroaryl hydroxy compound, a monocarboxylic acid amide, a pyridine compound, and a thienoxicam compound. Tenoxicam is an anti-inflammatory drug with analgesic and antipyretic effects used to treat osteoarthritis and control acute pain.
Indications For the treatment of rheumatoid arthritis, osteoarthritis, back pain, and general pain. Mechanism of Action The anti-inflammatory effect of tenoxicam may stem from its inhibition of cyclooxygenase, which in turn inhibits the synthesis of peripheral prostaglandins. Since prostaglandins sensitize pain receptors, inhibiting prostaglandin synthesis is the reason tenoxicam exerts its peripheral analgesic effect. Its antipyretic effect may be achieved through a central mechanism acting on the hypothalamus, leading to peripheral vasodilation and increased skin blood flow, thereby resulting in heat dissipation. Pharmacodynamics Tenoxicam is an anti-inflammatory drug with analgesic and antipyretic effects, used to treat osteoarthritis and control acute pain. Tenoxicam is a NSAID that inhibits COX-1 and COX-2 enzymes, reducing prostaglandin synthesis. It is used to treat osteoarthritis, rheumatoid arthritis, and acute pain. The drug is approved for clinical use in many countries. Its molecular formula is C13H11N3O4S2, and its molecular weight is 337.37. It is also known by the brand name Tilcotil. |
| Molecular Formula |
C13H11N3O4S2
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| Molecular Weight |
337.3741
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| Exact Mass |
337.019
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| CAS # |
59804-37-4
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| Related CAS # |
Tenoxicam-d3
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| PubChem CID |
54677971
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.7±0.1 g/cm3
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| Melting Point |
209-2130ºC
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| Index of Refraction |
1.741
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| LogP |
1.52
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
599
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LZNWYQJJBLGYLT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H11N3O4S2/c1-16-10(13(18)15-9-4-2-3-6-14-9)11(17)12-8(5-7-21-12)22(16,19)20/h2-7,17H,1H3,(H,14,15,18)
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| Chemical Name |
4-hydroxy-2-methyl-1,1-dioxo-N-pyridin-2-ylthieno[2,3-e]thiazine-3-carboxamide
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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) |
DMSO : ~50 mg/mL (~148.21 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.41 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 (7.41 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (7.41 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 | 2.9641 mL | 14.8205 mL | 29.6410 mL | |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL | |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 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 |
| NCT02549118 | Unknown status | Drug: Tenoxicam Drug: Pethidine |
Analgesia Obstetrical |
Ain Shams Maternity Hospital | 2015-09 | Phase 2 |
| NCT04182191 | Completed | Drug: Tenoxicam | Molar, Third Pain |
University of Sao Paulo | 2018-03-01 | Phase 4 |
| NCT05508451 | Completed | Procedure: Double jaw surgery | Postoperative Pain, Acute | TC Erciyes University | 2018-04-01 | Not Applicable |
| NCT05497570 | Completed | Drug: Tenoxicam Injectable Product | Arthrocentesis | Ataturk University | 2019-05-03 | Phase 1 |
| NCT02160236 | Unknown status | Drug: dexketoprofen trometamol Drug: tenoxicam Drug: serum physiologic |
Postoperative Pain | TC Erciyes University | 2014-11 | Phase 4 |
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