| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Sudoxicam targets cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2, which are responsible for the synthesis of prostaglandins from arachidonic acid. By inhibiting COX enzymes, sudoxicam reduces the production of prostaglandins, which are mediators of inflammation, pain, and fever. This mechanism is the basis for its anti-inflammatory, analgesic, and antipyretic effects.
|
|---|---|
| ln Vitro |
Human liver microsomes exhibit covalent binding to sudoxicam that is reliant on NADPH. Glutathione (GSH) blocks around half of the covalent integration of sudoxicam when added to microsome incubations [1]. In NADPH-supplemented human liver microsomes, metabolite identification investigations of [14C]-suldoxicam reveal that the primary metabolic pathway entails P450-mediated breakage of the thiazole ring to produce the matching acylthiourea molecule (S3), which is an adult protoxin[1]. Oxidative thiazole open biotransformation of sudoxicam occurs in vitro, producing acyl thioureas and their subsequent hydroxylated metabolites [3].
In vitro, sudoxicam demonstrates anti-inflammatory activity by inhibiting COX enzymes. It exhibits anti-edema and antipyretic properties. As an NSAID, it is used in research to study inflammation and pain mechanisms. |
| ln Vivo |
Rats treated with oral sudoxicam (1–10 mg/kg) once daily for seven days saw a significant decrease in plasma inflammatory units, a reduction in the swelling of inflamed hind paws, and a return to normal daily weight gain[2]. Even at oral dosages of 0.1 mg/kg, sudoxicam dramatically prevents the onset of edema in intact rats [2]. In guinea pigs, sudoxicam prevents erythema brought on by UV exposure. animals given an intraperitoneal injection of the typhoid/paratyphoid vaccine can develop a fever, whereas animals given sudoxicam (3.3 mg/kg, ip) can avoid this fever and remain at the same body temperature as rats given no injection [2]. Sudoxicam has a plasma half-life of eight hours in monkeys, thirteen hours in rats, and sixty hours in dogs [2].
In vivo, sudoxicam is used as an anti-inflammatory agent. It has been studied for its potential in treating various inflammatory conditions. However, its development as a therapeutic agent may have been limited due to its side effect profile. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for sudoxicam typically involve evaluating its inhibitory activity against purified COX-1 and COX-2 enzymes. The enzyme is incubated with varying concentrations of sudoxicam and a substrate such as arachidonic acid. The reaction is monitored by measuring the production of prostaglandins, and the IC₅₀ is determined.
|
| Cell Assay |
For in vitro cell-based assays, sudoxicam is dissolved in DMSO and applied to cultured cells such as macrophages or synoviocytes at concentrations ranging from 1-100 µM. The effects on prostaglandin production, inflammatory cytokine expression, and cell viability are assessed after 1-24 hours of treatment.
|
| Animal Protocol |
Animal/Disease Models: injected, i>M rats. Butyric acid [2]
Doses: 1 mg/kg, 3.3 mg/kg, 10 mg/kg Route of Administration: oral; daily; for 7 days. Experimental Results: All can effectively reduce plasma inflammatory units and reduce swelling of inflamed hind paws. In vivo animal studies for sudoxicam are typically conducted in rodent models of inflammation, such as the carrageenan-induced paw edema model or the adjuvant-induced arthritis model. Sudoxicam is administered orally or intraperitoneally at doses ranging from 1-50 mg/kg. Efficacy is evaluated by measuring paw swelling, pain response, and levels of inflammatory markers. |
| ADME/Pharmacokinetics |
Sudoxicam has a molecular formula of C₁₃H₁₁N₃O₄S₂ and a molecular weight of 337.37 g/mol. It is a white to off-white powder. It is soluble in DMSO and is typically stored as a powder at -20°C.
|
| Toxicity/Toxicokinetics |
Sudoxicam is considered to have a manageable toxicity profile consistent with other NSAIDs. Common side effects include gastrointestinal disturbances, such as nausea, vomiting, and abdominal pain. The risk of gastrointestinal bleeding and ulceration is associated with NSAID use. Renal toxicity and cardiovascular risks are also associated with NSAIDs.
|
| References | |
| Additional Infomation |
Sudoxicam is a nonsteroidal anti-inflammatory drug (NSAID) belonging to the oxicam class. It is a reversible COX antagonist with anti-inflammatory, anti-edema, and antipyretic properties. Sudoxicam is not approved for clinical use and is intended for research purposes only. It is supplied by various research chemical suppliers for non-human use.
|
| Molecular Formula |
C13H11N3O4S2
|
|---|---|
| Molecular Weight |
337.37
|
| Exact Mass |
337.019
|
| CAS # |
34042-85-8
|
| PubChem CID |
54682951
|
| Appearance |
Off-white to yellow solid powder
|
| Density |
1.675g/cm3
|
| Melting Point |
240-243 °C (dec.)
|
| Index of Refraction |
1.741
|
| LogP |
2.734
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
22
|
| Complexity |
599
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
SYCHUQUJURZQMO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H11N3O4S2/c1-16-10(12(18)15-13-14-6-7-21-13)11(17)8-4-2-3-5-9(8)22(16,19)20/h2-7,17H,1H3,(H,14,15,18)
|
| Chemical Name |
4-hydroxy-2-methyl-1,1-dioxo-N-(1,3-thiazol-2-yl)-1λ6,2-benzothiazine-3-carboxamide
|
| Synonyms |
EINECS 251-808-7; CP-15,973; Sudoxicam
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~247.00 mM)
|
|---|---|
| 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 | 2.9641 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
