COX-2-IN-30
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1160498-08-7
- Formel: C17H16N6O3S
- Molecular Weight:384.41
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
COX-2 49 nM (IC50) |
COX-1 10.4 μM (IC50) |
hCA I 183.4 nM (Ki) |
hCA II 81.4 nM (Ki) |
hCA IX 38.4 nM (Ki) |
hCA XII 21.6 nM (Ki) |
5-LOX 2.4 μM (IC50) |
In Vitro
COX-2-IN-30 (compound 7a) binds to hCA isoforms with Ki values of 183.4 nM (hCA I), 81.4 nM (hCA II), 38.4 nM (hCA IX), 21.6 nM (hCA XII), respectively[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-30 (10 mg/kg; po; single dose) results a significant reduction of paw height in Carrageenan (HY-125474)-induced rat paw edema assay. And COX-2-IN-30 siginificantly decreases the levels of TNF-α and IL-1β[1].
COX-2-IN-30 (10 mg/kg; po; 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.
-
Animal Model:Albino mice (25-30 g)[1]
-
Dosage:10 mg/kg
-
Administration:PO; single dose; after one hour, 0.1 mL of 1 percent acetic acid in a volume of 0.1 mL/10 g body weight was used to produce writhing.
-
Result:Decreased the number of writhing responses of mouse conpared with control group.
-
Animal Model:Paw edema rat induced by Carrageenan (HY-125474)[1]
-
Dosage:10 mg/kg
-
Administration:PO; single dose; after one hour, 0.1 mL of 1% carrageenan solution was injected in the left hind paw; measure inflammation height at 0, 1, 2, and 3 h
-
Result:Showed a significant reduction of paw height compared to control after 3 h.
Chemical Information
-
CAS. Nr. 1160498-08-7
-
Molecular Weight 384.41
-
Formel C17H16N6O3S
-
SMILES
O=C(C1=C(N(N=C1)C2=CC=C(C=C2)S(N)(=O)=O)N)N/N=C/C3=CC=CC=C3
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
-
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.
-
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
Verweise
[1]. Ragab MA, et al. 4-(5-Amino-pyrazol-1-yl)benzenesulfonamide 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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
COX-2-IN-30 Related Classifications
HY-149269 Related Classifications
Powered by Bioz