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-N1380S
    Guaiacol-d7
    Guaiacol-d7 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.
    Guaiacol-d<sub>7</sub>
  • HY-121235S1
    Clonixin-13C,d3
    		Inhibitor
    Clonixin-13C,d3 (SCH-10304-13C,d3) is the deuterium and 13C-labeled Clonixin (HY-121235). Clonixin is an orally active non-steroidal anti-inflammatory agent (NSAID) that inhibits COX synthesis. Clonixin acts as a voltage-gated L-type calcium channel blocker, exerts vasodilatory effects by antagonizing Ca2+ in vascular smooth muscle. Clonixin inhibits TGF-β, reduces lung coefficient, immune cell infiltration level, oxidative stress response, airway resistance, hydroxyproline content and collagen deposition. Clonixin can be used in research related to inflammation such as idiopathic pulmonary fibrosis and moderate to severe pain.
    Clonixin-<sup>13</sup>C,d<sub>3</sub>
  • HY-N0147R
    Rutaecarpine (Standard)
    		Inhibitor
    Rutaecarpine (Standard) is the analytical standard of Rutaecarpine. This product is intended for research and analytical applications. Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).
    Rutaecarpine (Standard)
  • HY-161513
    iNOS/COX-2-IN-1
    		Inhibitor
    iNOS/COX-2-IN-1 (Compound 12e) is an inhibitor of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). iNOS/COX-2-IN-1 inhibits the NF-κB and MAPKs signaling pathways and thus exerts anti-inflammatory effects.
    iNOS/COX-2-IN-1
  • HY-N6908R
    Continentalic acid (Standard)
    		Inhibitor
    Continentalic acid (Standard) is the analytical standard of Continentalic acid (HY-N6908). This product is intended for research and analytical applications. Continentalic acid is a diterpenoid organic acid. Continentalic acid exhibits multiple activities including anti-inflammatory, antioxidant, neuroprotective, antibacterial and antitumor effects. Continentalic acid alleviates oxidative stress, reduces pro-inflammatory cytokine production, inhibits MAPK phosphorylation and neutrophil infiltration, and induces growth inhibition and apoptosis of cancer cells. Continentalic acid can be used in research related to traumatic brain injury, cancer, inflammation and infections.
    Continentalic acid (Standard)
  • HY-N13040
    Isoscoparin-7-O-glucoside
    		Inhibitor
    Isoscoparin-7-O-glucoside is a flavonoid compound found in barley leaves. The total phenolic content (TPC) of isoscoparin-7-O-glucoside is positively correlated with COX-2 inhibitory activity, indicating anti-inflammatory activity. Isoscoparin-7-O-glucoside can be used in the study of inflammation.
    Isoscoparin-7-O-glucoside
  • 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-159634
    Zidometacin
    		Inhibitor
    Zidometacin is a nonsteroidal anti-inflammatory agent. Zidometacin significantly inhibits prostaglandin synthesis with low gastrolesive influence. Zidometacin has antinociceptive and antipyretic activities and shows relatively low ulcerogenicity in rat models. Zidometacin can be used for analgesia and osteoarthritis research.
    Zidometacin
  • 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-173518
    SIN 14
    		Inhibitor
    SIN 14, a derivative of Sinomenine (HY-15122), is an orally active HO-1 activator (KD = 17.2 μM). SIN 14 binds to the catalytic core domain of HO-1 and induces HO-1 activation in catalysis. SIN 14 significantly increases HO-1 stability. SIN 14 has anti-inflammatory effects and inhibits M1 macrophage polarization while promoting M2 polarization in LPS (Lipopolysaccharides)(HY-D1056)-induced RAW264.7 cells. SIN 14 inhibits inflammatory mediator production (eg: NO, IL-6, IL-1β and CCL2, inhibits production of ROS and down-regulates the expression of COX-2 and iNOS. SIN 14 can inhibit RA-related inflammatory edema in collagen-induced arthritis (ClA) mice.
    SIN 14
  • 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-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-181155
    Anti-inflammatory agent 111
    		Inhibitor
    Anti-inflammatory agent 111 is a potent anti-inflammatory agent. Anti-inflammatory agent 111 reduces Lipopolysaccharides (LPS) (HY-D1056)-induced i-NOS and COX-2 protein expression, decreases nitric oxide, IL-6, and TNF-α production. Anti-inflammatory agent 111 maintains normal cell viability at bioactive concentrations.Anti-inflammatory agent 111 can be used for the research of inflammation-related disorders.
    Anti-inflammatory agent 111
  • 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-N17888
    Ephemeranthol A
    		Inhibitor
    Ephemeranthol A is a phenanthrene compound with anticancer and anti-inflammatory activities. Ephemeranthol A exerts significant anti-inflammatory effects in macrophages by inhibiting the NF-κB and MAPK signaling pathways. Ephemeranthol A induces apoptosis and inhibits metastasis of lung cancer cells by suppressing the FAK/Akt signaling and EMT processes. Ephemeranthol A can be used for the research of acute and chronic inflammatory diseases and non-small cell lung cancer.
    Ephemeranthol A
  • 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 98.9%
    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>
Cat. No. Product Name / Synonyms Application Reactivity
COX Isoform Comparison

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