Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Pharmacological inhibition of COX can provide relief from the symptoms of inflammation and pain. Drugs, like Aspirin, that inhibit cyclooxygenase activity have been available to the public for about 100 years. Two cyclooxygenase isoforms have been identified and are referred to as COX-1 and COX-2. Under many circumstances the COX-1 enzyme is produced constitutively (i.e., gastric mucosa) whereas COX-2 is inducible (i.e., sites of inflammation). Non-steroidal anti-inflammatory drugs (NSAID), such as aspirin and ibuprofen, exert their effects through inhibition of COX. The main COX inhibitors are the non-steroidal anti-inflammatory drugs (NSAIDs).
|Cat. No.||Product Name||CAS No.||Information|
A non-steroidal anti-inflammatory drug (NSAID); primarily indicated as a pre-operative anti-miotic as well as orally for arthritis or dental pain; cyclooxygenase (COX) inhibitor.
Acetaminophen is a well-known analgesic and antipyretic agent that selectively inhibits COX activities in the brain; might modulate the endogenous cannabinoid system in the brain through paracetamol's metabolite, AM404; is typically used for mild to moderate pain.
PTUPB is a novel dual acting COX-2/sEH inhibitor with IC50 of 1.26 uM/0.9 nM,does not inhibits COX-1 (IC50>100 uM); reduces kidney injury parameters, decreases inflammatory and oxidative stress markers in ZDF rats; exhibits more effective than the same dose of either COX-2 inhibitor (celecoxib) or sEH inhibitor (t-AUCB) alone, shows in vivo antiallodynic activity in vivo; also suppresses glioblastoma growth by targeting EGFR and hyaluronan mediated motility receptor, potentiates the antitumor efficacy of cisplatin.
Vitacoxib is a potent, selective COX-2 inhibitor with IC50 of 0.34 ug/mL, >50-fold selectivity over COX-1 (IC50=19.4 ug/mL); a novel nonsteroidal anti-inflammatory drugs for veterinary use.
Ibuprofen ((±)-Ibuprofen) is a non-selective, reversible COX inhibitor with IC50 of 1 ug/mL and 46 ug/mL for COX-1 and COX-2 in enzyme assay, respectively; converts arachidonic acid to prostaglandin H2 (PGH2); is used for treating pain, fever, and inflammation.
Rofecoxib (MK-0996;MK-966) is a potent, selective and orally active COX-2 inhibitor with IC50 of 26 nM for inhibition of the COX-2-dependent production of PGE2 in human osteosarcoma cells; displays 1,000-fold selectivity over COX-1 activity; selectively inhibits LPS-induced, COX-2-derived PGE(2) synthesis after blood coagulation (IC50=0.53 uM); exhibits anti-inflammation activity in osteoarthritis and rheumatoid arthritis rodent models.
SC-236 (SC58236) is a potent, selective, orally active inhibitor of COX-2 with IC50 of 10 nM; displays >1,700-fold selectivity over COX-1 (IC50=17.8 uM); exhibits anti-inflammatory properties and potent antimetastatic activity both in vitro and in vivo.
NCX-4016 (Nitroaspirin;NO-Aspirin 1) is a nitroderivative of aspirin that combines cyclooxygenase inhibitor with an NO donor, directly and irreversiblely inhibits COX-1; suppresses platelet activation, platelet aggregation and thromboxane A2 production, reduces infarct size caused by myocardial ischemia-reperfusion in the anesthetized rat.
Tilmacoxib (JTE-522) is a potent, selective inhibitor of cyclooxygenase-2 (COX-2) that inhibits human recombinant COX-2 with IC50 of 85 nM, dispalys no activity against COX-1 (IC50>100 uM); significantly inhibits fibrosis, also inhibits growth of pulmonary metastases of colorectal cancer in rats.
Parecoxib(SC-69124A) is a potent and selective COX-2 inhibitor; a water-soluble prodrug of valdecoxib.
No.1378 West Wenyi Road, Yuhang District, HangZhou, Zhejiang, China