COX-2-IN-31
COX-2-IN-31 (compound 7b) is an orally active and dual inhibitor of COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM). COX-2-IN-31 also inhibits transmembrane hCA IX(Ki=48.9 nM) and hCA XII(Ki=5.8 nM) activity. COX-2-IN-31 exhibits anti-inflammatory and analgesic activity.
For research use only. We do not sell to patients.
- CAS No.: 3039955-76-2
- Formula: C17H16N6O4S
- Molecular Weight:400.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
COX-1 12.5 μM (IC50) |
COX-2 60 nM (IC50) |
In Vitro
COX-2-IN-31 (compound 7b) potently inhibits hCA IX and XII with Ki values in the nanomolar range(48.9 nM and 5.8 nM) in the Carbonic anhydrase inhibition assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
COX-2-IN-31 (10 mg/kg; oral gavage; single dose) results a significant reduction of paw height in Carrageenan (HY-125474)-induced rat paw edema assay[1].
COX-2-IN-31 (10 mg/kg; p.o; single dose) shows safety profile on the gastric tissues in male albino rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acetic acid writhing test in mice[1]
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Dosage:10 mg/kg
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Administration:Oral gavage; single dose; 1 h.
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Result:Decreased the number of writhing responses of mouse conpared with control group.
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Animal Model:Carrageenan (HY-125474)-induced rat paw edema[1]
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Dosage:10 mg/kg
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Administration:Oral gavage:; single dose; 1-3h
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Result:Decreased the edema volume of mouse conpared with control group.
Chemical Information
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CAS No. 3039955-76-2
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Molecular Weight 400.41
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Formula C17H16N6O4S
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SMILES
NC1=C(C=NN1C2=CC=C(C=C2)S(N)(=O)=O)C(N/N=C/C3=CC=C(C=C3)O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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
References
[1]. Ragab MA, et al. 4-(5-Amino-pyrazol-1-yl) benzene sulfonamide derivatives as novel multi-target anti-inflammatory agents endowed with inhibitory activity against COX-2, 5-LOX and carbonic anhydrase: Design, synthesis, and biological assessments. Eur J Med Chem. 2023 Mar 15; 250:115180. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)