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).
COX Isoform Specific Products
All Product Categories
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COX Related Products (1315)
Related Products (1315)
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Antibodies (6)
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COX Isoform Comparison
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Salicylic acid-13C6
0 ImagesCat. No.: HY-B0167S1CAS No.: 1189678-81-6Synonyms: 2-Hydroxybenzoic acid-13C6Salicylic 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.
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Rebamipide mofetil
0 ImagesCat. No.: HY-109158CAS No.: 1527495-76-6Rebamipide 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.
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Diflunisal-d3
0 ImagesSynonyms: MK-647-d3Diflunisal-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.
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Tolfenamic Acid (Standard)
0 ImagesSynonyms: GEA 6414 (Standard)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.
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Phoxim
0 ImagesCat. No.: HY-B0819CAS No.: 14816-18-3Phoxim is an organophosphorus pesticide and an orally active inhibitor of cholinesterase and CYP3A, which induces neurotoxicity in Caenorhabditis elegans and causes nephrotoxicity characterized by glomerular atrophy and interstitial fibrosis. Phoxim induces inhibition of the autophagy pathway. Phoxim induces dopaminergic neuron degeneration and exacerbates Aβ-induced paralysis. Phoxim damages enterocytes and disrupts intestinal barrier integrity. Phoxim induces ROS accumulation. Phoxim induces mitochondrial apoptosis, involving upregulation of Bad, Bax, caspase-3, and caspase-9 and downregulation of Bcl-2. Phoxim inhibits mitochondrial functional enzymes (COX, Ca2+-Mg2+-ATPase, SDH). Phoxim upregulates Nrf2 mRNA expression in the jejunal mucosa. Phoxim increases TNF-α and decreases IL-6 and IL-8 in the intestinal mucosa. Phoxim alters gut microbial composition by increasing total bacteria and Escherichia coli and reducing Lactobacillus. Phoxim enhances energy metabolism in silver carp by upregulating key glycolytic and gluconeogenic enzymes. Phoxim is used in research on neurodegenerative diseases, nephrotoxicity, intestinal oxidative stress and barrier dysfunction, and bacterial sepsis.
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Nepafenac-d5
0 ImagesSynonyms: AHR-9434-d5; AL-6515-d5Nepafenac-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 PGE₂. 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.
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Cimicoxib
0 ImagesSynonyms: UR-8880Cimicoxib (UR-8880) is an orally active, blood-brain barrier-permeable COX-2 inhibitor that also exerts targeted inhibition on CYP2D15. It has an IC50 of 66 nM against hCOX-2, an IC50 of 1.6 μM against canine CYP2D15, and an IC50 of 0.056 μM against feline CYP2D15. By inhibiting the COX-2 pathway to reduce the production of thromboxane B2 and prostaglandin E2, Cimicoxib exerts antipyretic, anti-inflammatory and analgesic effects. Cimicoxib is metabolized by CYP2D15 to form demethyl-cimicoxib, undergoes glucuronidation via UDP-glucuronosyltransferases, and exhibits biphasic elimination kinetics in beagle dogs. Cimicoxib is widely used in studies of inflammatory diseases, osteoarthritis, and perioperative pain associated with orthopedic or soft tissue surgeries.
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PPOH
0 ImagesPPOH, 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.
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3,9-Dihydroeucomin
0 ImagesCat. No.: HY-137011CAS No.: 887375-68-03,9-Dihydroeucomin (compound 12) is a natural homoisoflavonoid compound with less COX-2 inhibitory activitys.
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Gliquidone-d6
0 ImagesCat. No.: HY-B1114SSynonyms: AR-DF 26-d6Gliquidone-d6 (AR-DF 26-d6) is the deuterated-labeled Gliquidone (HY-B1114). Gliquidone can bind to the pancreatic β-cells and increases insulin release to regulate blood glucose levels. Gliquidone significantly decreases LPS (HY-D1056)-induced proinflammatory responses and inhibits ERK/STAT3/NF-κB phosphorylation in BV2 microglial cells. Gliquidone can suppress microgliosis, microglial hypertrophy mediated by LPS, and proinflammatory cytokine COX-2 and IL-6 levels in murine model. Gliquidone also exhibits good anticancer activity in lung carcinoma cells. Gliquidone has antioxidant property. Gliquidone can be studied in research for type 2 diabetes and cancers.
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Naproxen etemesil
0 ImagesSynonyms: LT-NS 001; MX 1094
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Ampyrone (Standard)
0 ImagesAmpyrone (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.
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Tryptanthrin (Standard)
0 ImagesTryptanthrin (Standard) is the analytical standard of Tryptanthrin. This product is intended for research and analytical applications. Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α.
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Guluronic acid
0 ImagesCat. No.: HY-N7700CAS No.: 15769-56-9Synonyms: G2013Guluronic acid (G2013) is an orally active oxidative stress regulator and anti-inflammatory agent that exerts pharmacological effects by down-regulating various pro-inflammatory and oxidative stress-related genes (such as TLR4, NF-κB, iNOS, etc.) and inhibiting the activities of COX-2, MMPs and VEGF. Low-dose Guluronic acid up-regulates the expression of immunoregulatory genes SHIP1 and SOCS1, thereby effectively inhibiting cancer-related inflammation, tumor angiogenesis, cell adhesion and metastasis, while reducing the accumulation of immunosuppressive cells. Guluronic acid significantly prolongs the survival time of tumor-bearing hosts within a concentration range without direct cytotoxicity, demonstrating favorable safety. Guluronic acid has involved in the research of multiple sclerosis, ankylosing spondylitis, breast cancer and other inflammatory diseases.
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Cucurbitacin R
0 ImagesCat. No.: HY-N11080CAS No.: 55903-92-9Cucurbitacin R is an orally active anti-inflammatory agent. Cucurbitacin R is isolated from the roots of Cayaponia tayuya. Cucurbitacin R inhibits Cyclooxygenase-2. Cucurbitacin R inhibits Interleukin-6-induced STAT3 activation and cytokine production, blocks NF-κB activation, and selectively prevents NFAT nuclear translocation without affecting Calcineurin activity. Cucurbitacin R inhibits TNF-α production and Nitric-oxide synthase-2 expression. Cucurbitacin R reduces joint damage, soft tissue swelling, paw edema, ear edema, inflammatory cell infiltration, and epithelial thickness. Cucurbitacin R can be used for research on arthritis and delayed-type hypersensitivity.
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Hydralazine-d4 (hydrochloride)
0 ImagesCat. No.: HY-B0464SCAS No.: 2749234-32-8Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain.
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Ibuprofen-13C6
0 ImagesCat. No.: HY-78131S3CAS No.: 1216459-54-9Synonyms: (±)-Ibuprofen-13C6Ibuprofen-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.
