Isoxicam
Based on 1 Customer Validation
Isoxicam is an orally active nonsteroidal anti-inflammatory compound and a COX-1/COX-2 inhibitor. Isoxicam exhibits potent anti-inflammatory activity in rat models of inflammation and significantly lower ulcerogenic risk. Isoxicam can be used for the study of inflammatory diseases and rheumatic disorders.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.83%
- CAS. Nr.: 34552-84-6
- Formel: C14H13N3O5S
- Molecular Weight:335.34
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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HY-14166
MK-886FLAP Inhibitor -
HY-13568
BenoxaprofenNonsteroidal Anti-inflammatory Agent -
HY-B1130R
Isoxicam (Standard)COX Inhibitor -
HY-B0641
FelbinacNon-steroidal Anti-Inflammatory Agent -
HY-14166R
MK-886 (Standard)FLAP Inhibitor -
HY-B0641R
Felbinac (Standard)Non-steroidal Anti-Inflammatory Agent -
HY-13568R
Benoxaprofen (Standard)Anti-inflammatory/Antipyretic Compound
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
COX-1 |
COX-2 |
In Vivo
Isoxicam (0.391-50 mg/kg; p.o.; daily, alternate days; days 1-20, days 14-27) exhibits dose-dependent prophylactic and therapeutic anti-arthritic activity in adjuvant-induced polyarthritis in rats, with prolonged activity detectable after treatment cessation[2].
Isoxicam (125-1000 mg/kg; p.o.) has significantly lower gastric and intestinal ulcerogenic potential than comparator anti-inflammatory drugs, with gastric ulcer incidence ED50 252 mg/kg and intestinal ulcer incidence ED50 822 mg/kg, showing no mortality at tested doses[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Charles River (Sprague-Dawley derived) (male, 150 g); Charles River (Sprague-Dawley derived) adrenalectomized (male, 150 g, used 1 week post-operation, maintained on 0.9% saline or hydrocortisone acetate 0.25 mg/animal)[2]
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Dosage:6.25 mg/kg; 12.5 mg/kg; 25.0 mg/kg; 50.0 mg/kg
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Administration:p.o.
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Result:Inhibited carrageenin-induced rat paw edema by 4-45% at 6.25-50.0 mg/kg when dosed 1, 3, 19, or 24 hours before challenge.
Reduced edema by 24% at 25 mg/kg in adrenalectomized rats and by 65% when combined with hydrocortisone acetate.
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Animal Model:Charles River-Lewis (male, 150 g)[2]
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Dosage:0.391 mg/kg; 1.56 mg/kg; 3.12 mg/kg; 6.25 mg/kg; 25.0 mg/kg; 50.0 mg/kg
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Administration:p.o.; daily (days 1-20, days 14-27); alternate days (days 1-20, days 14-27)
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Result:Improved body weight gain and reduced hind paw weight, thymus atrophy, and adrenal hypertrophy in a dose-dependent manner under daily prophylactic dosing at 1.56, 6.25, and 25.0 mg/kg.
Attenuated hind paw swelling and organ weight abnormalities under alternate-day prophylactic dosing at 1.56, 6.25, and 25.0 mg/kg.
Diminished body weight loss and hind paw edema under daily and alternate-day therapeutic dosing at 1.56, 6.25, and 25.0 mg/kg.
Retained significantly lower hind paw displacement than phenylbutazone at 6.25, 25, and 50 mg/kg on days 28, 35, and 42 after cessation of prophylactic dosing.
Maintained detectable plasma levels 37-42% lower at 48 h than at 24 h after alternate-day dosing at 6.25 and 25.0 mg/kg.
Showed no significant effects at 0.391 mg/kg in the prophylactic regimen.
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Animal Model:Charles River (Sprague-Dawley derived) (male, 145-200 g, 24-hour fasted, gastric ulcer evaluation)
Charles River (Sprague-Dawley derived) (male, 180 g, intestinal ulcer evaluation)[2] -
Dosage:125 mg/kg; 250 mg/kg; 500 mg/kg; 1000 mg/kg
700 mg/kg; 800 mg/kg; 900 mg/kg; 1000 mg/kg -
Administration:p.o.
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Result:Induced gastric ulceration with 40% incidence at 125 mg/kg and 100% incidence at 1000 mg/kg, yielding gastric ulcer ED50 of 252 mg/kg and severity EDom of 333 mg/kg.
Produced intestinal ulceration with 17% incidence at 700 mg/kg and 100% incidence at 1000 mg/kg, yielding intestinal ulcer ED50 of 822 mg/kg and severity EDom of 1009 mg/kg.
Chemical Information
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CAS. Nr. 34552-84-6
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Appearance Solid
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Molecular Weight 335.34
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Formel C14H13N3O5S
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Color White to off-white
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SMILES
O=C(C1=C(O)C2=CC=CC=C2S(N1C)(=O)=O)NC3=NOC(C)=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 3.33 mg/mL (9.93 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Cotton Pellet Granuloma
Cotton pellet granuloma is a classical in vivo chronic inflammation model used to evaluate the anti-inflammatory potential of test substances by measuring their ability to inhibit granuloma tissue formation around an implanted foreign body (cotton pellet) in rodents. The method is based on the biological response to a sterile implanted material, which induces proliferative phase inflammation characterized by fibroblast proliferation and collagen-rich granuloma formation, and the final readout reflects the extent of chronic inflammatory tissue growth surrounding the pellet. In multiple preclinical pharmacological evaluations, inhibition of cotton pellet-induced granuloma formation has been used as an indicator of anti-inflammatory activity in both synthetic and natural product screening contexts.
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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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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
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 2.9820 mL | 14.9102 mL | 29.8205 mL | 74.5512 mL |
| 5 mM | 0.5964 mL | 2.9820 mL | 5.9641 mL | 14.9102 mL |
Isoxicam Related Classifications
HY-B1130 Related Classifications
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