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-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
    		Inhibitor
    Benoxaprofen-13C, d3 is the 13C-labeled Benoxaprofen (HY-13568). Benoxaprofen (LRCL 3794) is a nonsteroidal anti-inflammatory agent that blocks the biosynthesis of inflammatory mediators such as leukotrienes and prostaglandins by inhibiting 5-LOX, PGH2 synthase and cytochrome P-450. Benoxaprofen exhibits significant toxicity: it not only alters cellular redox status, uncouples oxidative phosphorylation and disrupts calcium ion homeostasis, but also causes liver injury through the formation of covalent adducts between its active metabolites and hepatic proteins. Benoxaprofen shows strong phototoxicity under ultraviolet irradiation, and induces erythrocyte lysis, mast cell degranulation and histamine release. Benoxaprofen is widely used in studies of urticaria and related phototoxic mechanisms.
    Benoxaprofen-<sup>13</sup>C,d<sub>3</sub>
  • HY-178454
    Multitarget AD-IN-3
    		Inhibitor
    Multitarget AD-IN-3 is a brain-penetrant neuroprotective agent. Multitarget AD-IN-3 can selectively inhibit MAO-B with an IC50 of 4.42 μM and a SI of 18.12. Multitarget AD-IN-3 can eliminate ROS. Multitarget AD-IN-3 Multitarget AD-IN-3 can inhibit Aβ1-42 self-aggregation and can reverse Aβ1-42-induced mitochondrial membrane depolarization and inhibit apoptosis. Multitarget AD-IN-3 can be used for the research of neurological disease, such as Alzheimer’s disease.
    Multitarget AD-IN-3
  • 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-183187
    4H-Chromen-4-one-o-carborane
    		Inhibitor
    4H-Chromen-4-one-o-carborane is an estrogen receptor (ER) agonist, with an EC50 of 0.9 μM for ERα and an EC50 of 11.1 μM for ERβ. 4H-Chromen-4-one-o-carborane also acts as an inhibitor of COX-1 and COX-2, with an IC50 of 6.6 μM for COX-1 and an IC50 of 17.7 μM for COX-2.
    4H-Chromen-4-one-o-carborane
  • 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-N1326
    Santamarine
    		98.85%
    Santamarine (Santamarin; Balchanin) is a sesquiterpene lactone found in Artemisia scoparia. Santamarine shows anti-inflammatory, antioxidant, anticancer and anti-photoaging activities. Santamarine suppresses UVA-induced phosphorylation of JNK and p38 MAPK, nuclear translocation of phosphorylated c-Fos and c-Jun, and AP-1-mediated MMP-1 transcription and secretion. Santamarine suppresses NF-κB signaling, iNOS, COX-2, TNF-α, and IL-1β production. Santamarine inhibits thioredoxin reductase activity, induces ROS production, mitochondrial apoptosis, G2/M cell cycle arrest, and DNA damage, and reduces cancer cell growth. Santamarine can be used for the photoaging, inflammatory diseases and cancer.
    Santamarine
  • HY-177643B
    Lixadesiran sodium scrambled negative control
    		Inhibitor
    Lixadesiran sodium scrambled negative control is the sequence scrambled negative control of Lixadesiran sodium.
    Lixadesiran sodium scrambled negative control
  • HY-N16849
    Myristinin A
    		Inhibitor
    Myristinin A (YM 26567-1) is a trans-isomer flavan compound found in Horsfieldia amygdaline and Myristica cinnamomea. Myristinin A can selectively inhibit COX-2 activity with an IC50 of 16.9 μg/mL. Myristinin A can reduce the production of prostaglandin E2 (PGE2) and inhibit phospholipase A2 (PLA2), thereby blocking the release of inflammatory mediators. Myristinin A can inhibit Candida albicans with an IC50 of 8.8 μg/mL. Myristinin A can be used for the research of inflammation and infection, such as rheumatoid arthritis.
    Myristinin A
  • 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
  • HY-162244
    COX-2-IN-40
    		Inhibitor
    COX-2-IN-40 (compound 17) is a COX-2 inhibitor with the IC50 of 14.86 μM. COX-2-IN-40 can be used for study of chronic pain.
    COX-2-IN-40
  • HY-W002116S
    Methyl syringate-d6
    		Inhibitor
    Methyl syringate-d6 is the deuterium labeled Methyl syringate. Methyl syringate is a selective TRPA1 agonist. Methyl syringate regulates food intake and gastric emptying through a TRPA1-mediated pathway. Methyl syringate is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a chemical marker of Asphodel monofloral honey. Methyl syringate contributes to the antibacterial activity of honey. Methyl syringate inhibits aflatoxin production. Methyl syringate can contribute to weight suppression. Methyl syringate can be studies for cancer prevention (e.g. lung cancer), suppression of hypoxia-induced inflammatory response and tumorigenesis.
    Methyl syringate-d<sub>6</sub>
  • HY-150721
    COX-2-IN-29
    		Inhibitor
    COX-2-IN-29 (Compound 15b) is a selective and orally active COX-2 inhibitor with an IC50 of 0.005 μM.
    COX-2-IN-29
  • HY-163188
    COX-2/LOX-IN-2
    		Inhibitor
    COX-2/LOX-IN-2 (compound 6) is a dual inhibitor of COX-2/LOX with IC50s of 7.0 μM and 27.5 μM, respectively. COX-2/LOX-IN-2 has antioxidant activity and has the potential to be used in the development of nonsteroidal anti-inflammatory drugs (tNSAIDs).
    COX-2/LOX-IN-2
  • HY-B0335S1
    Tolfenamic acid-13C6
    		Inhibitor 99.7%
    Tolfenamic acid-13C6 is the 13C6 labeled Tolfenamic acid. 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-<sup>13</sup>C<sub>6</sub>
  • HY-N0747R
    Oxypeucedanin (Standard)
    		Inhibitor
    Oxypeucedanin (Standard) is a furanocoumarin derivative found in Angelica dahurica. Oxypeucedanin (Standard) is an orally active PI3K/AKT/NF-κB, MAPK, and ROS inhibitor. Oxypeucedanin (Standard) induces cell cycle arrest and apoptosis. Oxypeucedanin (Standard) inhibits hKv1.5 channel currents (IC50: 76 nM). Oxypeucedanin (Standard) exhibits anticancer, anti-inflammatory, antioxidant and antiarrhythmic activities.
    Oxypeucedanin (Standard)
  • HY-14931
    Naproxcinod
    		Inhibitor
    Naproxcinod (Nitronaproxen) is the first in class of cyclooxygenase (COX)-inhibiting nitric oxide donators (CINODs). Naproxcinod shows analgesic and anti-inflammatory effects, it can be used for the research of osteoarthritis and inflammation.
    Naproxcinod
  • HY-B0574S
    Mefenamic acid-d4
    		Inhibitor 98.0%
    Mefenamic acid-d4 is a deuterium labeled Mefenamic acid. Mefenamic acid is a BBB-permeable non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
    Mefenamic acid-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity
COX Isoform Comparison

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