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

COX

Cyclooxygenase

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 Effect Purity Chemical Structure
  • HY-15036A
    Diclofenac diethylamine
    Inhibitor 99.95%
    Diclofenac diethylamine is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
    Diclofenac diethylamine
  • HY-N2736
    3′,4′,7-Trihydroxyflavone
    Inhibitor 98.0%
    3′,4′,7-Trihydroxyflavone is an orally active inhibitor of OXA-48 (IC50 = 1.89 μM) and COX-1 (IC50 = 36.37 μM). 3′,4′,7-Trihydroxyflavone exhibits antioxidant and anti-inflammatory properties, inhibiting the release of inflammatory cytokines such as IL-6, IL-8, and TNF-α. 3′,4′,7-Trihydroxyflavone inhibits H2O2-induced neuronal apoptosis and ROS accumulation, and exerts anti-neuroinflammatory effects by suppressing the JNK-STAT1 pathway. 3′,4′,7-Trihydroxyflavone exhibits antimicrobial and antibiotic-modifying activities against multidrug-resistant Gram-negative enteric bacteria. 3′,4′,7-Trihydroxyflavone inhibits RANKL-induced osteoclast formation via NFATc1. 3′,4′,7-Trihydroxyflavone activates the CREB-BDNF axis and restores scopolamine (HY-N0296)-induced memory deficits in mice.
    3′,4′,7-Trihydroxyflavone
  • HY-B0568R
    Deferiprone (Standard)
    Inhibitor
    Deferiprone (Standard) is the analytical standard of Deferiprone. This product is intended for research and analytical applications. Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study.
    Deferiprone (Standard)
  • HY-N7148S1
    γ-Tocopherol-d4
    Inhibitor 98.90%
    γ-Tocopherol-d4 is the deuterium labeled γ-Tocopherol. γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity.
    γ-Tocopherol-d<sub>4</sub>
  • HY-15321S
    Etoricoxib-d4
    98.82%
    Etoricoxib-d4 (MK-0663-d4) is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
    Etoricoxib-d<sub>4</sub>
  • HY-15036R
    Diclofenac (Standard)
    Inhibitor
    Diclofenac (Standard) is the analytical standard of Diclofenac. This product is intended for research and analytical applications. Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
    Diclofenac (Standard)
  • HY-N2459
    Peonidin chloride
    Inhibitor 98.70%
    Peonidin chloride is an O-methylated anthocyanidin that functions as a primary plant pigment, endowing purplish-red hues to flowers such as the peony, from which it takes its name, as well as berries and vegetables. Peonidin chloride exhibits chemopreventive, as well as anti-inflammatory activities on cancer cells in vitro, blocking COX-2 expression and transformation in JB6 P+ mouse epidermal cells.
    Peonidin chloride
  • HY-A0259
    Floctafenine
    Inhibitor
    Floctafenine, a nonsteroidal anti-inflammatory agent (NSAID), acts as an effective analgesic agent. Floctafenine is an inhibitor of COX-1 and COX-2 activities in vitro,showing a slightly higher potency towards COX-I. Floctafenine is used for the research of short term pain research.
    Floctafenine
  • HY-B1054
    Famprofazone
    Inhibitor 98.38%
    Famprofazone is a non-steroidal anti-inflammatory drug (NSAID) that belongs to the pyrazolone series, and it has analgesic, anti-inflammatory, and antipyretic effects.
    Famprofazone
  • HY-131258
    Ibuprofen impurity 1
    Inhibitor 98.0%
    Ibuprofen impurity 1 is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
    Ibuprofen impurity 1
  • HY-114950
    EXP3179
    Inhibitor 98.09%
    EXP3179 is an important intermediate aldehyde metabolite of Losartan. EXP3179 has no AT1-R–blocking activity, but potently inhibits the expression of endothelial cyclooxygenase (COX)-2. EXP3179 exerts potent anti-inflammatory actions.
    EXP3179
  • HY-17357S
    Nepafenac-d5
    Inhibitor 98.84%
    Nepafenac-d5 (AHR-9434-d5; AL-6515-d5) is the deuterium labeled Nepafenac (HY-17357). Nepafenac, a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.
    Nepafenac-d<sub>5</sub>
  • HY-113445
    Thromboxane B3
    Thromboxane B3 is a prostaglandin analog derived from arachidonic acid (AA) in the cyclooxygenase (COX) metabolic pathway. Thromboxane B3 is generated from arachidonic acid (AA) in platelets and vascular endothelial cells through the catalysis of cyclooxygenase (COX) and thromboxane synthase (TXS). Thromboxane B3 has been reported to be formed by human platelets upon ingestion of eicosapentaenoic acid (C20: 5ω3).
    Thromboxane B3
  • HY-106579
    Tiaprofenic acid
    Inhibitor 99.93%
    Tiaprofenic acid is an orally active nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory and analgesic potency. Tiaprofenic acid inhibits prostaglandin synthesis by suppressing cyclo-oxygenase (COX). Tiaprofenic acid can be used in the treatment of rheumatic diseases.
    Tiaprofenic acid
  • HY-W012817
    Methylhydroquinone
    Inhibitor 99.91%
    Methylhydroquinone is an orally active COX inhibitor with IC50s of 480.7 μM and 52.2 μM for ovine COX-1 and human recombinant COX-2, respectively. Methylhydroquinone has potential DNA damaging effects: 1) inhibiting COX-1 to reduce prostaglandin synthesis and exert anti-inflammatory activity; 2) inducing DNA single-strand breaks. Methylhydroquinone exerts its effects by competitively binding to the active sites of COX-1 (such as Tyr385, Met522) and non-covalent interactions.
    Methylhydroquinone
  • HY-14654S1
    Aspirin-d4
    Inhibitor
    Aspirin-d4 is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
    Aspirin-d<sub>4</sub>
  • HY-17361
    Etofenamate
    Inhibitor 98.35%
    Etofenamate, a non-steroid anti-inflammatory agent (NSAID) and a non-selective COX inhibitor, possesses analgesic, anti-rheumatic, antipyretic and anti-inflammatory properties. Etofenamate is used in the research for osteoarthritis, arthritis and other inflammatory diseases.
    Etofenamate
  • HY-B0714
    Dexketoprofen (trometamol)
    Inhibitor 99.73%
    Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective COX inhibitor. Dexketoprofen trometamol has a pain-relieving effect, anti-inflammatory effect and anti-cancer effect.
    Dexketoprofen (trometamol)
  • HY-W087194
    p-Ethylhydratropic acid
    Control 99.60%
    p-Ethylhydratropic acid (compound 5b) is the impurity of Ibuprofen (HY-78131). Ibuprofen is a potent, orally active, selective COX-1 inhibitor.
    p-Ethylhydratropic acid
  • HY-B0261R
    Meloxicam (Standard)
    Inhibitor
    Meloxicam (Standard) is the analytical standard of Meloxicam. This product is intended for research and analytical applications. Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 μM and 36.6 μM for COX-2 and COX-1, respectively.
    Meloxicam (Standard)
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