| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
Droxicam targets cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2. As a prodrug, it is converted to its active form, piroxicam, in the body. Piroxicam inhibits the conversion of arachidonic acid to prostaglandins, thereby reducing inflammation, pain, and fever.
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| ln Vitro |
In vitro, droxicam is a weak inhibitor of COX enzymes, as it is a prodrug. Its activity is primarily due to its conversion to piroxicam. Piroxicam is a potent inhibitor of both COX-1 and COX-2.
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| ln Vivo |
In edema caused by carrageenan, droxicam (0.25 and 0.5 mg/kg; interface) shows strong anti-inflammatory effect [1]. When it comes to modelin-induced edema in tumors, doxicam (ED50, po; 5, 6, 7, 8 h; 7.5, 12.9, 4.8, 8.4 mg/kg) has strong anti-inflammatory efficacy [1]. Mycobacterium butyricum had good antiarthritic activity in scaffolds against initial and secondary reactions when Droxicam (ED50, oral, 1, 2, 3, 4 hours: 0.51, 0.94, 1.56, 4.88 mg/kg) was injected. Styrylquinone sensor, microphone cholinergic sensor Droxicam (ED50=0.081 mg/kg; po) Protective pathway kinase, ED50 are 5.3 mg/kg and 1.1 mg/kg, respectively[1]. Peritoneal capillary permeability[1] caused the mice to writhe, and Droxicam demonstrated the greatest analgesic activity in preventing this behavior. In the Irwin test, mice's behavior at 80 mg/kg, ip, and 160 mg/kg, po, is not affected by dronicam [1]. In anesthetized cats, droxicam does not cause uric acid excretion in the channel activity, nor does it affect the cats' responses to histamine, nordepinephrine, or choline in the cardiovascular or respiratory systems [1].
In vivo, droxicam is used as an NSAID to reduce inflammation and pain in conditions like rheumatoid arthritis and osteoarthritis. It is administered orally and is converted to piroxicam in the body, which then exerts its therapeutic effects. |
| Enzyme Assay |
In vitro enzyme assays for droxicam are not typically performed, as it is a prodrug. The activity of its active metabolite, piroxicam, is measured using standard COX inhibition assays. COX-1 and COX-2 enzymes are incubated with arachidonic acid and various concentrations of the inhibitor. Prostaglandin production is measured by ELISA or other methods.
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| Cell Assay |
For in vitro cellular assays, cells such as macrophages or fibroblasts are used. The cells are stimulated with an inflammatory stimulus (e.g., LPS) to induce prostaglandin production. Various concentrations of droxicam or its active metabolite are added, and prostaglandin levels in the culture media are measured.
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| Animal Protocol |
In vivo animal studies for droxicam are conducted in standard models of inflammation, such as the carrageenan-induced paw edema model in rats. The compound is administered orally, and the reduction in paw swelling is measured. Its analgesic effects are assessed in models like the writhing test.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Time to Peak (Tmax) is 7 hours. Bioavailability is comparable to [DB00554], which, based on rabbit data, is considered to be completely absorbed in humans. Prodrug Data Unavailable. See [DB00554] for information on the active compound. Prodrug Data Unavailable. See [DB00554] for information on the active compound. Prodrug Data Unavailable. See [DB00554] for information on the active compound. Metabolism/Metabolite Converted to [DB00554] via ester hydrolysis. Biological Half-Life Prodrug Data Unavailable. See [DB00554] for information on the active compound. Droxicam has a molecular weight of 447.46 g/mol and a molecular formula of C21H22N4O5S. It is a solid. It is typically stored at room temperature. |
| Toxicity/Toxicokinetics |
Protein Binding
Prodrug data are unavailable. For information on the active compound, please refer to [DB00554]. Droxicam is generally well-tolerated, but like other NSAIDs, it can cause gastrointestinal side effects such as nausea, dyspepsia, and ulcers. It may also cause headache, dizziness, and fluid retention. It should be used with caution in patients with a history of peptic ulcer disease or renal impairment. |
| References |
[1]. Farré AJ, et al. Pharmacological properties of droxicam, a new non-steroidal anti-inflammatory agent. Methods Find Exp Clin Pharmacol. 1986 Jul;8(7):407-22.
[2]. Jané F, et al. Droxicam: a pharmacological and clinical review of a new NSAID. Eur J Rheumatol Inflamm. 1991;11(4):3-9. |
| Additional Infomation |
Droxicam is an organic heterocyclic tricyclic compound with the chemical name 2H,5H-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione-6,6-dioxide, in which the 3 and 5 positions are substituted with pyridin-2-yl and methyl groups, respectively. It is a prodrug of piroxicam, used to relieve pain and inflammation caused by musculoskeletal diseases such as rheumatoid arthritis and osteoarthritis. It possesses various pharmacological activities, including as a prodrug, nonsteroidal anti-inflammatory drug (NSAID), cyclooxygenase-1 inhibitor, non-narcotic analgesic, platelet aggregation inhibitor, and hepatotoxic agent. It belongs to the pyridine class of compounds and is an organic heterocyclic tricyclic compound. It is functionally related to piroxicam. Doloxicam is an oxacinoid NSAID and a prodrug of [DB00554]. It is used to relieve pain and inflammation caused by musculoskeletal diseases such as rheumatoid arthritis and osteoarthritis.
Drug Indications Droxicam is a nonsteroidal anti-inflammatory drug (NSAID) previously used to treat inflammation and rheumatoid arthritis.Mechanism of Action Droxicam is converted to [DB00554] in the intestine via ester hydrolysis. Administration of droxicam inhibits the synthesis of prostaglandins by cyclooxygenase.Pharmacodynamics Droxicam is a prodrug of [DB00554]. Administration of droxicam produces similar anti-inflammatory, antirheumatic, analgesic, and antipyretic effects as [DB00554]. Droxicam is a prodrug of the NSAID piroxicam. It is used for the treatment of rheumatoid arthritis, osteoarthritis, and other inflammatory conditions. |
| Molecular Formula |
C16H11N3O5S
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|---|---|
| Molecular Weight |
357.34
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| Exact Mass |
357.041
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| CAS # |
90101-16-9
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| PubChem CID |
65679
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
554.7±60.0 °C at 760 mmHg
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| Melting Point |
259-261°
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| Flash Point |
289.3±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.748
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| LogP |
1.11
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
25
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| Complexity |
741
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1C2=NC=CC=C2)OC(C3=CC=CC=C34)=C(N(C)S4(=O)=O)C1=O
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| InChi Key |
OEHFRZLKGRKFAS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H11N3O5S/c1-18-13-14(10-6-2-3-7-11(10)25(18,22)23)24-16(21)19(15(13)20)12-8-4-5-9-17-12/h2-9H,1H3
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| Chemical Name |
5-methyl-6,6-dioxo-3-pyridin-2-yl-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4-dione
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| Synonyms |
Droxicamum Droxicam
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.7985 mL | 13.9923 mL | 27.9846 mL | |
| 5 mM | 0.5597 mL | 2.7985 mL | 5.5969 mL | |
| 10 mM | 0.2798 mL | 1.3992 mL | 2.7985 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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