Ampiroxicam
Based on 2 publication(s) in Google Scholar
Ampiroxicam is an orally active prodrug of non-steroidal anti-inflammatory drug (NSAID). Ampiroxicam inhibits paw swelling in adjuvant-induced arthritis and acute inflammation models, and suppresses phenylbenzoquinone-induced stretching responses in mice. Ampiroxicam is rapidly and completely converted to Piroxicam (HY-B0253) via non-specific esterases and first-pass metabolism. Ampiroxicam induces contact hypersensitivity and photosensitivity reactions through photoproducts generated by UVA. Ampiroxicam can be used in research related to photosensitivity, adjuvant-induced arthritis, rheumatism, osteoarthritis and other inflammatory diseases.
For research use only. We do not sell to patients.
- Purity : 98.73%
- CAS No.: 99464-64-9
- Formula: C20H21N3O7S
- Molecular Weight:447.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Ampiroxicam
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Biological Activity
Description
IC50 & Target
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COX |
Parmacokinetics
| Species | Dose | Route | AUC | Bioavailability | Cmax | Tmax |
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| Rat[2] | 10 mg/kg | p.o. | / | / | 26 μg/mL | 4 h |
| Rat[2] | 3.2 mg/kg | p.o. | 126 μg·h/mL | 91 % | 12 μg/mL | 2 h |
| Rat[2] | 3.2 mg/kg | i.v. | 125 μg·h/mL | 91 % | / | / |
| Dog[2] | 1.0 mg/kg | p.o. | 99 μg·h/mL | 72 % | 2.5 μg/mL | 1.5 h |
| Dog[2] | 1.0 mg/kg | i.v. | 108 μg·h/mL | 78 % | / | / |
| Monkey[2] | 5.0 mg/kg | p.o. | 207 μg·h/mL | 52 % | 16 μg/mL | 2 h |
| Monkey[2] | 5.0 mg/kg | i.v. | 280 μg·h/mL | 54 % | / | / |
In Vivo
Ampiroxicam (1-4.1 mg/kg; p.o.; single dose) inhibits the stretching response in fasted CF-1 mice induced by benzoquinone, with an MPE50 of 2.0 mg/kg[2].
Ampiroxicam (4.3-41 mg/kg; p.o.; single daily dose for 5 days) inhibits carrageenan-induced hind paw edema in fasted Sprague-Dawley rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hartley (female, 380-450 g, contact hypersensitivity model via adjuvant patch test modified maximization method)[1]
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Dosage:1% (UVA-irradiated, sensitization); 1% (UVA-irradiated, challenge); 1% (thiosalicylate challenge)
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Administration:topical occlusive patch; daily for 3 consecutive days (primary sensitization); topical occlusive patch; single dose on day 9 (repeat sensitization); topical open application; single dose on day 21 (challenge)
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Result:Induced a mean total skin reaction score of 3.3 (5/5 animals positive) when challenged with UVA-irradiated 1% ampiroxicam.
Induced a mean total skin reaction score of 4.7 (5/5 animals positive) when challenged with 1% thiosalicylate.
Induced a mean total skin reaction score of 4.0 (4/5 animals positive) with UVA (25.5 J/cm2)-irradiated 1% ampiroxicam challenge.
Showed no positive reactions to non-irradiated 1% ampiroxicam, UVA-irradiated 1% piroxicam, or non-irradiated 1% piroxicam.
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Animal Model:CF-1 (fasted overnight, N ≥5/group)[2]
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Dosage:1.0-4.1 mg/kg
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Administration:oral gavage; single dose
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Result:Determined an MPE50 of 2.0 mg/kg (95% confidence interval 1.0-4.1 mg/kg) for suppression of phenylbenzoquinone-induced stretching.
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Animal Model:Sprague-Dawley (fasted, N ≥6/group)[2]
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Dosage:4.3-41 mg/kg
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Administration:oral; single dose; oral; daily; 5 days
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Result:Determined an ED50 of 28 mg/kg (95% confidence interval 21-41 mg/kg) for single oral dose administration.
Determined an ED50 of 7.8 mg/kg (95% confidence interval 4.3-28 mg/kg) for 5 consecutive daily oral doses.
Chemical Information
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CAS No. 99464-64-9
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Appearance Solid
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Molecular Weight 447.46
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Formula C20H21N3O7S
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Color White to off-white
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SMILES
O=C(OC(OC(C1=CC=CC=C12)=C(C(NC3=NC=CC=C3)=O)N(C)S2(=O)=O)C)OCC
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Synonyms
CP 65703
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (111.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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Carrageenan-Induced Paw Edema
Carrageenan-induced paw edema is an acute inflammation model in which intraplantar injection of carrageenan induces localized inflammatory swelling characterized by vascular permeability, leukocyte infiltration, and production of inflammatory mediators such as prostaglandins and cytokines, making it widely used to evaluate anti-inflammatory agents in vivo. The resulting paw volume or thickness increase is quantified over time as a direct readout of inflammatory intensity and drug efficacy, typically reflecting cyclooxygenase-mediated prostaglandin-driven edema formation and immune cell recruitment in peripheral tissue[20].
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Zymosan-Induced Peritonitis
Zymosan-induced peritonitis is a sterile acute-inflammation model produced by intraperitoneal injection of zymosan, a yeast cell-wall particle preparation, followed by quantification of leukocyte recruitment and soluble inflammatory mediators in peritoneal lavage fluid. Low-dose zymosan peritonitis is commonly used as a self-resolving acute inflammation model in which neutrophil recruitment occurs early and monocyte/macrophage accumulation follows later. The assay readouts include total peritoneal leukocyte number, differential neutrophil and monocyte/macrophage counts, peritoneal cytokines and chemokines, plasma or peritoneal exudation, and optional lipidomic or metabolomic changes during inflammation and resolution. Early neutrophil recruitment after zymosan depends strongly on complement and mast-cell C5a receptor signaling, whereas later monocyte recruitment is linked to MCP-1/CCL2 production.
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Contact Hypersensitivity Dermatitis
Contact hypersensitivity (CHS) dermatitis is a T cell-mediated delayed-type (Type IV) immune reaction in which low-molecular-weight haptens applied to the skin bind host proteins to form complete antigens, triggering sensitization followed by a secondary inflammatory response upon re-exposure (elicitation phase), which is commonly quantified by ear swelling as a readout of skin inflammation in murine models. This model is widely used to study allergic contact dermatitis because it is antigen-specific, reproducible, and reflects key immunological events including dendritic cell activation, T cell priming in draining lymph nodes, and effector T cell-driven tissue inflammation. DNFB- and oxazolone-induced CHS models are standard systems for evaluating both acute and chronic T cell-dependent skin inflammation and for testing immunomodulatory interventions.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Sasaki T, et al. Antigenic characterization in ampiroxicam-induced photosensitivity using an in vivo model of contact hypersensitivity. J Dermatol Sci. 1999;21(3):170-175. [Content Brief]
[2]. Carty TJ, et al. Ampiroxicam, an anti-inflammatory agent which is a prodrug of piroxicam. Agents Actions. 1993;39(3-4):157-165. [Content Brief]
[3]. Ogiso T, et al. Pharmacokinetic drug interactions between ampiroxicam and sulfaphenazole in rats. Biol Pharm Bull. 1999;22(2):191-196. [Content Brief]
[4]. Kurumaji Y. Ampiroxicam-induced photosensitivity. Contact Dermatitis. 1996 Apr;34(4):298-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2348 mL | 11.1742 mL | 22.3484 mL | 55.8709 mL |
| 5 mM | 0.4470 mL | 2.2348 mL | 4.4697 mL | 11.1742 mL | |
| 10 mM | 0.2235 mL | 1.1174 mL | 2.2348 mL | 5.5871 mL | |
| 15 mM | 0.1490 mL | 0.7449 mL | 1.4899 mL | 3.7247 mL | |
| 20 mM | 0.1117 mL | 0.5587 mL | 1.1174 mL | 2.7935 mL | |
| 25 mM | 0.0894 mL | 0.4470 mL | 0.8939 mL | 2.2348 mL | |
| 30 mM | 0.0745 mL | 0.3725 mL | 0.7449 mL | 1.8624 mL | |
| 40 mM | 0.0559 mL | 0.2794 mL | 0.5587 mL | 1.3968 mL | |
| 50 mM | 0.0447 mL | 0.2235 mL | 0.4470 mL | 1.1174 mL | |
| 60 mM | 0.0372 mL | 0.1862 mL | 0.3725 mL | 0.9312 mL | |
| 80 mM | 0.0279 mL | 0.1397 mL | 0.2794 mL | 0.6984 mL | |
| 100 mM | 0.0223 mL | 0.1117 mL | 0.2235 mL | 0.5587 mL |