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-B1130
    Isoxicam
    Inhibitor 99.83%
    Isoxicam is an orally active, long-acting, non-steroidal anti-inflammatory agent for the research of arthritis. Isoxicam is a nonselective inhibitor of COX-1 and COX-2.
    Isoxicam
  • HY-B0230S2
    Phenylbutazone-13C12
    Inhibitor 99.90%
    Phenylbutazone-13C12 is the 13C12 labeled Phenylbutazone. Phenylbutazone is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Phenylbutazone, a hepatotoxin, is a nonsteroidal anti-inflammatory agent (NSAID). Phenylbutazone induces muscle blind-like protein 1 (MBNL1) expression and has the potential for ankylosing spondylitis research.
    Phenylbutazone-<sup>13</sup>C<sub>12</sub>
  • HY-B0167S1
    Salicylic acid-13C6
    Salicylic acid-13C6 is the 13C-labeled Salicylic acid (HY-B0167). Salicylic acid is a precursor to and a metabolite of Aspirin (HY-14654), can inhibit cyclo-oxygenase-2 (COX-2) activity.
    Salicylic acid-<sup>13</sup>C<sub>6</sub>
  • HY-109158
    Rebamipide mofetil
    Inhibitor
    Rebamipide mofetil is an orally active proagent of Rebamipide (OPC12759). Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner.
    Rebamipide mofetil
  • 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-N0416R
    Cucurbitacin B (Standard)
    Inhibitor
    Cucurbitacin B (Standard) is the analytical standard of Cucurbitacin B. This product is intended for research and analytical applications. Cucurbitacin B belongs to a class of highly oxidized tetracyclic triterpenoids and is oral active. Cucurbitacin B inhibits tumor cell growth, migration and invasion and cycle arrest, but induces cell apoptosis. Cucurbitacin B has potent anti-inflammatory, antioxidant, antiviral, hypoglycemic, hepatoprotective, neuroprotective activity.
    Cucurbitacin B (Standard)
  • HY-N6891
    Hamaudol
    Inhibitor 99.59%
    Hamaudol is a chromone isolated from Saposhnikovia divaricata. Hamaudol shows significant inhibitory activity on cyclooxygenase (COX)-1 and COX-2 activities with IC50 values of 0.30, 0.57 mM, respectively, and has potent analgesia and anti-inflammary effects.
    Hamaudol
  • HY-N8371
    Shizukaol B
    Inhibitor
    Shizukaol B is a lindenane-type dimeric sesquiterpene, used to be isolated from the whole plant of Chloranthus henryi. Shizukaol B has anti-inflammatory effect against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells. Shizukaol B inhibits iNOS and COX-2, and suppresses NO production, TNF-α, and IL-1β expression.
    Shizukaol B
  • HY-100516
    Cimicoxib
    Inhibitor 98.02%
    Cimicoxib (CX) is an orally active potent and selective COX-2 (cyclo-oxygenase-2) inhibitor. Cimicoxib exhibits promising anti-inflammatory and analgesic activity. The PK parameters of Cimicoxib in dogs given precise (2 mg/kg) and approximate doses (1.95-2.5 mg/kg) are similar.
    Cimicoxib
  • HY-N0569R
    Madecassic acid (Standard)
    Inhibitor
    Madecassic acid (Standard) is the analytical standard of Madecassic acid. This product is intended for research and analytical applications. Madecassic acid is isolated from Centella asiatica (Umbelliferae). Madecassic acid has anti-inflammatory properties caused by iNOS, COX-2, TNF-alpha, IL-1beta, and IL-6 inhibition via the downregulation of NF-κB activation in RAW 264.7 macrophage cells.
    Madecassic acid (Standard)
  • HY-119647
    PPOH
    Inhibitor 99.87%
    PPOH, a fatty acid derivative, is a selective cyclooxygenase (COX) inhibitor that inhibits arachidonic acid cyclooxygenase activity in renal cortical microsomes. In addition, PPOH acts on CYP4A2 and CYP4A3 with the IC50 values of 22 μM and 6.5 μM, respectively. PPOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PPOH
  • HY-137011
    3,9-Dihydroeucomin
    Inhibitor
    3,9-Dihydroeucomin (compound 12) is a natural homoisoflavonoid compound with less COX-2 inhibitory activitys.
    3,9-Dihydroeucomin
  • HY-W419589
    Xanthomicrol
    Inhibitor
    Xanthomicrol is extracted from the resin of the plant called Chinese bellflower (a member of the Scrophulariaceae family) and is a monoamine oxidase (MAOs) inhibitor. Xanthomicrol has anti-tumor and anti-inflammatory properties, with IC50 values of 0.88 and 1.69 μg/mL in HL60 and K562 cells. Xanthomicrol's the main metabolite of 5DT in mouse colon, and it can reduce levels of iNOS protein and mRNA, as well as COX-2 protein levels. Additionally, Xanthomicrol decreases the production of the pro-inflammatory cytokine IL-1β and induces the expression of the antioxidant enzyme HO-1.
    Xanthomicrol
  • HY-W121901
    Naproxen glucuronide
    98.71%
    Naproxen glucuronide ((S)-Naproxen-β-D-glucuronide) is a non-selective COX inhibitor. Naproxen glucuronide, a metabolite of naproxen, is a nonsteroidal anti-inflammatory drug (NSAID) of the propionic acid class (the same as ibuprofen) that relieves pain, fever, swelling, and stiffness.
    Naproxen glucuronide
  • HY-19675
    Naproxen etemesil
    Inhibitor 99.89%
    Naproxen etemesil is a lipophilic, non-acidic, inactive proagent of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
    Naproxen etemesil
  • HY-B1398R
    Ampyrone (Standard)
    Inhibitor
    Ampyrone (4-Aminophenazone) (Standard) is the analytical standard of Ampyrone (HY-B1398). This product is intended for research and analytical applications. Ampyrone (4-Aminophenazone; 4-Aminoantipyrine) is a reversible and low-damage optical clearing agent and non-selective COX inhibitor based on UV absorption properties. Ampyrone can improve the optical transmittance of mouse skin and other tissues. Ampyrone can induce tissue refractive index matching by enhancing UV absorption, reduce light scattering, and achieve tissue transparency in vivo. Ampyrone reduces the synthesis of prostaglandin PGE2, thereby exerting anti-inflammatory, analgesic and antipyretic effects. Ampyrone inhibits DNA damage, cell apoptosis and immune cell phagocytosis induced by Doxorubicin (HY-15142A) and Cisplatin (HY-17394), etc., and participates in the regulation of toxicity in tumor chemotherapy.
    Ampyrone (Standard)
  • HY-78131S3
    Ibuprofen-13C6
    Inhibitor
    Ibuprofen-13C6 ((±)-Ibuprofen-13C6) is a 13C labeled Ibuprofen (HY-78131). Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers.
    Ibuprofen-<sup>13</sup>C<sub>6</sub>
  • HY-105872
    Trifenagrel
    Inhibitor 99.35%
    Trifenagrel is an orally active platelet aggregation inhibitor that inhibits the inducing effects of arachidonic acid (AA) and collagen. The ED50s of trifenagrel for inhibiting AA- and collagen-induced platelet aggregation in guinea pigs were 1.4 mg/kg and 9.4 mg/kg, respectively.
    Trifenagrel
  • HY-N1965
    Gaultherin
    Inhibitor 99.44%
    Gaultherin is an orally active non-steroidal anti-inflammatory agent. Gaultherin selectively inhibits NF-κB, MAPK, COX-2 (IC50 = 0.35 mg/mL), LOX (IC50 = 0.56 mg/mL) and HYAL (IC50 = 28.58 μg/mL) to exert anti-inflammatory, antipyretic and analgesic effects. Gaultherin exhibits modest direct antioxidant capacity, greater in cell-based models. Gaultherin does not affect COX-1 so that avoids the common gastrointestinal side effects of Aspirin (HY-14654).
    Gaultherin
  • HY-U00129
    SC57666
    Inhibitor 98.94%
    SC57666 is a selective COX2 inhibitor with an IC50 of 26 nM.
    SC57666
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