2. Signaling Pathways
  3. Immunology/Inflammation
  4. COX

COX

Cyclooxygenase

COX

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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).

COX Isoform Specific Products:

COX Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W741411
    Tenoxicam-d4
    Tenoxicam-d4 (Ro-12-0068-d4) is the deuterium labeled Tenoxicam (HY-B0440). Tenoxicam (Ro-12-0068), an antiinflammatory agent with analgesic and antipyretic properties.
    Tenoxicam-d<sub>4</sub>
  • HY-115966
    COX-1/2-IN-1
    		Inhibitor
    COX-1/2-IN-2 is a potent COX1/2 inhibitor. COX-1/2-IN-2 exhibits significant inhibitory effect against COX-1 and COX-2 inhibitor with IC50 values of 13.9 ± 3.21 µM and 6.4±0.74 µM, respectively.
    COX-1/2-IN-1
  • HY-159562
    COX-2-IN-46
    		Inhibitor
    COX-2-IN-46 (compound 5m) is an anti-inflammatory agent with potent analgesic activity. COX-2-IN-46 exhibits a significant inhibitory effect on COX-2 (IC50=87.74 nM).
    COX-2-IN-46
  • HY-149270
    COX-2-IN-31
    		Inhibitor
    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.
    COX-2-IN-31
  • HY-N16129
    Diplacone
    		Inhibitor
    Diplacone (DP) is a geranylated flavanone. Diplacone can be isolated from the unripe fruits of Paulownia tomentosa. Diplacone has anti-inflammatory, antiradical, cytoprotective, antibacterial and anticancer activities. Diplacone induces ferroptosis-mediated cell death by increasing mitochondrial Ca2+ Influx, ROS production and mitochondrial permeability transition. Diplacone significantly inhibits AChE and BChE activity with IC50s of 7.2  μM and 1.4 μM for hAChE and BChE, respectively. Diplacone can be used for chronic inflammatory diseases like inflammatory bowel diseases (IBD), cancers like lung cancer and Alzheimer’s disease research.
    Diplacone
  • HY-W777079
    Valdecoxib-13C2,15N
    Valdecoxib-13C2,15N (SC 65872-13C2,15N) is the 13C- and 15N-labeled Valdecoxib (HY-15762). Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.
    Valdecoxib-13</sup>C<sub>2</sub>,15</sup>N<sub>
  • HY-115976
    COX-2-IN-10
    		Inhibitor
    COX-2-IN-10 is a potent COX-2 inhibitor. COX-2-IN-10 inhibits the production of PGE2 in concentration dependent manner (IC50=2.54 µM). COX-2-IN-10 inhibits the expression of iNOS and COX-2 on mRNA and protein level . COX-2-IN-10 inhibits the production of IL-6, TNF-α and IL-1β.
    COX-2-IN-10
  • HY-18763S
    Indobufen-d5
    		Inhibitor
    Indobufen-d5 is deuterium labeled Indobufen. Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes.
    Indobufen-d<sub>5</sub>
  • HY-N0908R
    Ginsenoside Rg5 (Standard)
    		Inhibitor
    Ginsenoside Rg5 (Standard) is the analytical standard of Ginsenoside Rg5. This product is intended for research and analytical applications. Ginsenoside Rg5 is the main component of Red ginseng and IGF-1R agonist. Ginsenoside Rg5 compets for the binding site of IGF-1R and blocks the binding of IGF-1 to IGF-1R (IC50 about 90 nM). Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
    Ginsenoside Rg5 (Standard)
  • HY-14398S1
    Celecoxib-d3
    		Inhibitor ≥99.0%
    Celecoxib-d3 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.
    Celecoxib-d<sub>3</sub>
  • HY-B0578AR
    Loxoprofen sodium (Standard)
    		Inhibitor
    Loxoprofen (sodium) (Standard) is the analytical standard of Loxoprofen (sodium). This product is intended for research and analytical applications. Loxoprofen sodium is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium can reduce atherosclerosis and shows antitumor activity.
    Loxoprofen sodium (Standard)
  • HY-B0905S
    Tilmicosin-d3
    		Inhibitor
    Tilmicosin-d3 is the deuterium labeled Tilmicosin. Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects.
    Tilmicosin-d<sub>3</sub>
  • HY-N4230
    Clematomandshurica saponin B
    		Inhibitor
    Clematomandshurica saponins B shows significant inhibitory activity on cyclooxygenase-2 (IC50=2.58 mM).
    Clematomandshurica saponin B
  • HY-N8641
    Kadsulignan N
    Kadsulignan N, a natural product has anti-HIV activity (EC50: 43.56 μM). Kadsulignan N is also a COX-2 ligand (Ki: 72.24 nM).
    Kadsulignan N
  • HY-N3716
    Dehydroglyasperin D
    		Inhibitor
    Dehydroglyasperin D inhibits rat and human Aldose Reductase (AR) (IC50: 62.4 μM and 176.2 μM respectively). Dehydroglyasperin D has anti-obesity, antioxidant effects. Dehydroglyasperin D shows anti-inflammatory activity by inhibiting COX-2 expression and the MLK3 signaling pathway. Dehydroglyasperin D also inhibits melanin synthesis. Dehydroglyasperin D is a prenylated flavonoid that can be isolated from Glycyrrhiza uralensi.
    Dehydroglyasperin D
  • HY-W775009R
    Imidazole salicylate (Standard)
    		Inhibitor
    Imidazole salicylate (Standard) is the analytical standard of Imidazole salicylate. This product is intended for research and analytical applications. Imidazole salicylate is a nonsteroidal anti-inflammatory drug that can be used to study cirrhosis and ascites.
    Imidazole salicylate (Standard)
  • HY-B0619S1
    Zaltoprofen-13C,d3
    		Inhibitor
    Zaltoprofen-13C,d3 is the 13C- and deuterium labeled Zaltoprofen. Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain.
    Zaltoprofen-<sup>13</sup>C,d<sub>3</sub>
  • HY-B2158S
    Chlorotrianisene-d9
    		Inhibitor
    Chlorotrianisene-d9 is the deuterium labeled Chlorotrianisene. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood.
    Chlorotrianisene-d<sub>9</sub>
  • HY-146704
    COX-2/sEH-IN-1
    		Inhibitor
    COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC50 values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks.
    COX-2/sEH-IN-1
  • HY-N12960
    Artobiloxanthone
    		Inhibitor
    Artobiloxanthone (Compound AA3) exhibits antitumor activity, particularly against oral squamous cell carcinoma (OSCC). Artobiloxanthone inhibits Akt/mTOR pathway and STAT3 pathway, inhibits proliferation of SAS and T.Tn (with IC50 of 11 and 22 μM), and inhibits the cancer cell migration. Artobiloxanthone arrests cell cycle at S phase, and induces apoptosis in OSCC cells through activation of caspase 3/9.
    Artobiloxanthone
Cat. No. Product Name / Synonyms Application Reactivity
COX Isoform Comparison

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