1. Signalwege
  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).

Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • 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-181056
    EGFR/COX-2-IN-3
    Inhibitor
    EGFR/COX-2-IN-3 is a selective EGFR/COX-2 dual inhibitor with IC50 values of 0.098 μM and 0.05 μM, respectively. EGFR/COX-2-IN-3 is predicted to have oral activity and blood-brain barrier permeability. EGFR/COX-2-IN-3 exhibits both potent analgesic activity and anti-glioblastoma effects. EGFR/COX-2-IN-3 can be used in the research of tumors such as glioblastoma.
    EGFR/COX-2-IN-3
  • HY-N17736
    Chikusetsusaponin IVa methyl ester
    Inhibitor
    Chikusetsusaponin IVa methyl ester (CME) is a natural triterpenoid saponin compound. Chikusetsusaponin IVa methyl ester induces G0/G1 cell cycle arrest and apoptosis in colon cancer cells by inhibiting the Wnt/β-catenin signaling pathway. By inhibiting the NF-κB and AP-1 signaling pathways, Chikusetsusaponin IVa methyl ester significantly reduces the production of NO, PGE₂ and pro-inflammatory cytokines (TNF-α, IL-6, IL-1β), and downregulates the levels of iNOS and COX-2. Chikusetsusaponin IVa methyl ester can be used in researches on colorectal cancer and inflammation.
    Chikusetsusaponin IVa methyl ester
  • 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-116243
    Vitacoxib
    Inhibitor
    Vitacoxib is an Imidazole (HY-D0837) derivative, selective COX-2 inhibitor, anti-inflammatory agent. Vitacoxib can be used in the research of inflammatory diseases, pain and fever.
    Vitacoxib
  • HY-177643A
    Lixadesiran sodium
    Inhibitor
    Lixadesiran sodium is a siRNA in STP705. It targets to COX-2. STP705 is composed of 2 siRNA oligonucleotides (Pixofisiran and Lixadesiran) that individually target TGF-β1 and COX-2 mRNA.
    Lixadesiran sodium
  • 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-181081
    CHNQD-03005
    Inhibitor
    CHNQD-03005 is an orally active anti-inflammatory agent. CHNQD-03005 inhibits the expression of iNOS and COX-2, reduces inflammatory signal transduction, suppresses NO production, and downregulates the pro-inflammatory cytokines TNF-α, IL-6 and IL-1β. CHNQD-03005 can be used in the research of inflammatory diseases such as colitis.
    CHNQD-03005
  • 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-17474S
    Parecoxib-d3
    Inhibitor
    Parecoxib-d3 is the deuterium labeled Parecoxib. Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
    Parecoxib-d<sub>3</sub>
  • HY-146371
    COX-2-IN-13
    Inhibitor
    COX-2-IN-13 (compound 13e) is a potent and selective inhibitor of COX-2 with an IC50 of 0.98 μM. COX-2-IN-13 is an anti-inflammatory agent. COX-2-IN-13 shows safety in-vivo acute toxicity study.
    COX-2-IN-13
  • HY-B0261A
    Meloxicam sodium
    Inhibitor
    Meloxicam sodium is a non-steroidal anti-inflammatory agent that can pass through the blood-brain barrier, inhibits COX activity, with IC50s of 0.49 μM and 36.6 μM for COX-2 and COX-1, respectively.
    Meloxicam sodium
  • HY-W007539R
    2,4-Dihydroxybenzaldehyde (Standard)
    Inhibitor
    2,4-Dihydroxybenzaldehyde (Standard) is the analytical standard of 2,4-Dihydroxybenzaldehyde. This product is intended for research and analytical applications. 2,4-Dihydroxybenzaldehyde is an endogenous metabolite. 2,4-Dihydroxybenzaldehyde is a pharmaceutical intermediate that can be used to synthesize various Schiff base compounds. 2,4-Dihydroxybenzaldehyde exhibits significant anti angiogenic, anti-inflammatory, and analgesic activities. 2,4-Dihydroxybenzaldehyde reduces the production of NO and ROS by inhibiting the expression of iNOS and COX-2. 2,4-Dihydroxybenzaldehyde is commonly used in the study of inflammatory conditions.
    2,4-Dihydroxybenzaldehyde (Standard)
  • HY-179142
    COX-2-IN-60
    Inhibitor
    COX-2-IN-60 is a potent, orally active, and selective COX-2 inhibitor with an IC50 of 0.06 μM. COX-2-IN-60 exhibits ~100-fold selectivity over COX-1 (IC50 = 5.93 ). COX-2-IN-60 reduces oxidative stress and neuroinflammatory cytokines, and effectively counteracts epileptogenesis. COX-2-IN-60 exhibits significant anticonvulsant effects and protects against hippocampal injury by suppressing oxidative stress (reducing MDA and NO), pro-inflammatory signaling (reducing TNF-α and IL-6), and glial activationin in the Pilocarpine (HY-B0726A)-induced seizure mouse model. COX-2-IN-60 can be used for the research on neuroinflammatory and epilepsy.
    COX-2-IN-60
  • HY-159564
    iNOS/COX-2-IN-3
    Inhibitor
    iNOS/COX-2-IN-3 (compound 7d) is a dual inhibitor of iNOS and COX-2, with potential anti-inflammatory activity against LPS (HY-D1056)-induced RAW 264.7 cells (IC50=3.48 μM). iNOS/COX-2-IN-3 has good plasma stability, oral activity and gastric safety, and its inhibitory activity on iNOS and COX-2 expression is 5.43-fold and 2.37-fold that of Indomethacin (HY-14397), respectively.
    iNOS/COX-2-IN-3
  • HY-15321R
    Etoricoxib (Standard)
    Inhibitor
    Etoricoxib (Standard) is the analytical standard of Etoricoxib. This product is intended for research and analytical applications. Etoricoxib (MK-0663) 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 (Standard)
  • HY-168070
    COX-2-IN-48
    Inhibitor
    COX-2-IN-48 (5-25), a COX-2 inhibitor with an IC50 of 51.7 nM for human COX-2, exerts anti-inflammatory and analgesic effects in various rodent models by inhibiting NF-κB pathway. COX-2-IN-48 (5-25) inhibits the degradation of IκB, the phosphorylation and nuclear translocation of NF-κB p65, and the expression of COX-2 and iNOS.
    COX-2-IN-48
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