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-B0808R
    Oxaprozin (Standard)
    		Inhibitor
    Oxaprozin (Standard) is the analytical standard of Oxaprozin. This product is intended for research and analytical applications. Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.
    Oxaprozin (Standard)
  • HY-N0261R
    Aurantio-obtusin (Standard)
    		Inhibitor
    Aurantio-obtusin (Standard) is the analytical standard of Aurantio-obtusin. This product is intended for research and analytical applications. Aurantio-obtusin is a anthraquinone compound that can be extracted from cassia seed. Aurantio-obtusin has the effects of decreasing blood pressure, decreasing blood lipids and anti-inflammatory.Aurantio-obtusin is an orally active vasodilator. Aurantio-obtusin ameliorates hepatic steatosis through AMPK/ autophagy-and AMPK/TFEB mediated inhibition of lipid accumulation.
    Aurantio-obtusin (Standard)
  • HY-119960
    AHR-10037
    		Inhibitor
    AHR-10037 is a non-steroidal anti-inflammatory agent with low gastric toxicity. AHR-10037 is a prodrug converted in vivo to a cyclooxygenase inhibitor.
    AHR-10037
  • HY-15029S2
    (±)-Naproxen-13C,d3
    (±)-Naproxen-13C,d3 is the deuterium and 13C labeled (±)-Naproxen. (±)-Naproxen ((Rac)-Naproxen) is a racemate of Naproxen (HY-15030). Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively.
    (±)-Naproxen-<sup>13</sup>C,d<sub>3</sub>
  • HY-159561
    COX-1-IN-2
    		Inhibitor
    COX-1-IN-2 (compound 5h) is an anti-inflammatory agent with potent analgesic activity. COX-1-IN-2 exhibits a significant inhibitory effect on COX-1 (IC50=38.76 nM).
    COX-1-IN-2
  • HY-B1456AS
    Fenoprofen-13C6 sodium hydrate
    		Inhibitor
    Fenoprofen-13C6 (LILLY-53858-13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
    Fenoprofen-<sup>13</sup>C<sub>6</sub> sodium hydrate
  • HY-146198
    COX-2-IN-19
    		Inhibitor
    COX-2-IN-19 (Compound 24) is a potent COX-2 inhibitor with an IC50 of 1.76 μM. COX-2-IN-19 shows in vivo anti-inflammatory activity.
    COX-2-IN-19
  • HY-115935
    COX-2-IN-8
    		Inhibitor
    COX-2-IN-8 (compound 6a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 6.585 uM. COX-2-IN-8 has higher COX-2 selectivity than Celecoxib. COX-2-IN-8 shows good in vivo anti-inflammatory and low ulcerogenic activity.
    COX-2-IN-8
  • HY-168888
    COX-2-IN-52
    		Inhibitor
    COX-2-IN-52 (Compound 5l) is an orally active and selective COX-2 inhibitor with an IC50 of 54 nM. COX-2-IN-52 can inhibit the release of NO in cells and has anti-inflammatory activity. COX-2-IN-52 has high gastrointestinal safety and can be used in the research of oral anti-inflammatory drugs.
    COX-2-IN-52
  • HY-155764
    COX-1/2-IN-4
    		Inhibitor
    COX-1/2-IN-4 (compound 2b) is anCOX inhibitorwith IC50 values of 0.239 μM and 0.191 μM for COX-1 enzyme and COX-2 enzyme , respectively. COX-1/2-IN-4showsmoderateanticanceractivity against COLO205 and B16F1 cancer cell lines with IC50 values of 30.79 and 74.15 μM, respectively.
    COX-1/2-IN-4
  • HY-18342S
    Diflunisal-d3
    		Inhibitor
    Diflunisal-d3 is the deuterium labeled Diflunisal. Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
    Diflunisal-d<sub>3</sub>
  • HY-150548
    COX-2/15-LOX-IN-1
    		Inhibitor
    COX-2/15-LOX-IN-1 (Compound 14) is a COX-2 and 15-lipoxygenase enzyme (15-LOX) inhibitor with IC50 values of 10.65, 0.075 and 2.98 μM against COX-1, COX-2 and 15-LOX, respectively. COX-2/15-LOX-IN-1 shows anti-inflammatory activity.
    COX-2/15-LOX-IN-1
  • HY-155133
    COX-2-IN-34
    		Inhibitor 98.87%
    COX-2-IN-34 (compound 8a) is a selective and orally active inhibitor of COX-2 , with an IC50 of 0.42 μM. COX-2-IN-34 has no gastric ulcer toxicity but has anti-inflammatory effects.
    COX-2-IN-34
  • HY-106579S
    Tiaprofenic acid-d3
    Tiaprofenic acid-d3 is a deuterium labeled Tiaprofenic acid. Tiaprofenic acid is a nonsteroidal anti-inflammatory agent (NSAID) mainly used in the treatment of rheumatic diseases.
    Tiaprofenic acid-d<sub>3</sub>
  • HY-W778179
    Benoxaprofen-13C,d3
    Benoxaprofen-13C,d3 (LRCL 3794-13C,d3) is the deuterium and 13C-labeled Benoxaprofen (HY-13568). Benoxaprofen (LRCL 3794) is a potent and long-acting anti-inflammatory and antipyretic compound. Benoxaprofen is a relatively weak inhibitor of cyclooxygenase in in vitro systems, inhibits lipoxygenase in other systems, and inhibits monocyte migration in some animal models of inflammation.
    Benoxaprofen-<sup>13</sup>C,d<sub>3</sub>
  • HY-B1355R
    Oxyphenbutazone monohydrate (Standard)
    		Inhibitor
    Oxyphenbutazone (monohydrate) (Standard) is the analytical standard of Oxyphenbutazone (monohydrate). This product is intended for research and analytical applications. Oxyphenbutazone monohydrate is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone monohydrate is an orally active non-selective COX inhibitor. Oxyphenbutazone monohydrate selectively kills non-replicating Mycobaterium tuberculosis.
    Oxyphenbutazone monohydrate (Standard)
  • HY-136720
    ZXX2-77
    		Inhibitor
    ZXX2-77 is a cyclooxygenase-1 (COX-1) selective inhibitor belonging to the benzenesulfonylanilide class of compounds. It is reported as a novel analgesic that does not cause gastric damage. ZXX2-77 has a weak analgesic effect but exhibits potent COX-1 inhibitory activity in vitro. The low oral absorption rate of ZXX2-77 leads to its weak analgesic effect in vivo. At a dose of 30 mg/kg, the maximum plasma concentration of ZXX2-77 (1.2 mM) did not reach its COX-1 IC50 value (3.2 mM). In contrast, its derivative ZXX2-79, although weaker in vitro COX inhibitory activity, is better absorbed, exhibits stronger analgesic effect and hardly causes gastric damage. These findings suggest that ZXX2-77 and its derivatives as COX-1 selective inhibitors may become effective analgesics that do not cause gastric damage.
    ZXX2-77
  • HY-W775009
    Imidazole salicylate
    		Inhibitor
    Imidazole salicylate is a nonsteroidal anti-inflammatory drug that can be used to study cirrhosis and ascites.
    Imidazole salicylate
  • HY-B0335R
    Tolfenamic Acid (Standard)
    		Inhibitor
    Tolfenamic Acid (Standard) is the analytical standard of Tolfenamic Acid. This product is intended for research and analytical applications. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
    Tolfenamic Acid (Standard)
  • HY-162425
    Anti-inflammatory agent 78
    		Inhibitor
    Anti-inflammatory agent 78 (compound L-37) is a potent anti-inflammatory agent. Anti-inflammatory agent 78 has significant potency on PGE2, PGE1, COX-2 and COX-1 inhibition. Anti-inflammatory agent 78 can inhibits NO release in LPS-stimulated RAW 264.7 cell line.
    Anti-inflammatory agent 78
Cat. No. Product Name / Synonyms Application Reactivity
COX Isoform Comparison

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