COX
Cyclooxygenase (COX) catalyzes the conversion of arachidonic acid into prostaglandin G2 and prostaglandin H2, initiating prostanoid biosynthesis that regulates inflammation, vascular homeostasis, pain signaling, and tissue responses to injury[1][2]. Mechanistically, COX enzymes contain two major isoforms, COX-1 and COX-2, which catalyze the same biochemical reaction but differ in gene regulation, tissue distribution, intracellular localization, and substrate selectivity[1][2]. COX-1 is constitutively expressed in most tissues and contributes to gastric mucosal protection, platelet function, and renal hemodynamic maintenance, whereas COX-2 is rapidly induced by inflammatory cytokines, growth factors, and pathological stimuli[1][3]. In disease models, increased COX-2 expression is associated with chronic inflammatory disorders, neurodegenerative diseases, and multiple cancer types, supporting its central role in inflammation-driven pathophysiology and tumor progression[1][2]. Compared with related isoforms, COX-2 contains a larger and more flexible substrate-binding channel that enables distinct inhibitor selectivity and broader fatty-acid utilization[1][4]. Therefore, selective and non-selective nonsteroidal anti-inflammatory drugs (NSAIDs) remain important experimental tools for dissecting prostaglandin-dependent signaling pathways, while COX-2-selective inhibitors have been widely used to investigate inflammatory mechanisms and disease-associated prostanoid production[1][2][4].
Références:
- [1]. Faki Y, et al. Different Chemical Structures and Physiological/Pathological Roles of Cyclooxygenases. Rambam Maimonides Med J. 2021 Jan 19;12(1):e0003. [Content Brief]
- [2]. Joanne P, et al. Lipid reorganization induced by membrane-active peptides probed using differential scanning calorimetry. Biochim Biophys Acta. 2009 Sep;1788(9):1772-81. [Content Brief]
- [3]. Cyclooxygenase in sciencedirect topic.
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COX Produits associés (740)
Produits associés (740)
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Roburic acid (Standard)
0 ImagesRoburic acid (Standard) is the analytical standard of Roburic acid. This product is intended for research and analytical applications. Roburic acid acts as an anti-inflammatory, anti-tumor and osteoclastogenesis inhibitor, with a Ki of 7.066 μM against human TNF, an IC50 of 9 μM against human COX-2, and an IC50 of 5 μM against ovine COX-1. Roburic acid reduces the production of inflammatory mediators such as NO and IL-6 in macrophages by inhibiting the NF-κB and MAPK (p38/JNK) pathways. By competitively inhibiting the TNF-TNF-R1 interaction, Roburic acid blocks the downstream NF-κB signaling pathway, thereby inducing cell cycle arrest and apoptosis in cancer cells. Roburic acid specifically inhibits osteoclastogenesis and bone resorption by suppressing the RANKL/TRAF6/NF-κB/NFATc1 axis. Roburic acid can be used in research related to osteolytic diseases such as osteoporosis, colorectal cancer and inflammatory diseases.
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Veratric acid (Standard)
0 ImagesVeratric acid (Standard) is the analytical standard of Veratric acid. This product is intended for research and analytical applications. Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant and anti-inflammatory activities. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.
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Ufenamate (Standard)
0 ImagesCat. No.: HY-100009RCAS No.: 67330-25-0Synonyms: Flufenamic acid butyl ester (Standard); Butyl flufenamate (Standard)Ufenamate (Standard) is the analytical standard of Ufenamate (HY-100009). This product is intended for research and analytical applications. Ufenamate (Flufenamic acid butyl ester) is an anthranilic acid-based anti-inflammatory drug that can be used in the study of skin diseases such as acute and chronic eczema, contact dermatitis, diaper dermatitis, miliary rashes and atopic dermatitis. Ufenamate has a certain photoprotective effect, reduces the degree of skin erythema and swelling in the photoaging model, downregulates the expression level of COX-2 and can promote the healing of mouse skull defects by secreting BMP2.
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Loxoprofen-d3
0 ImagesCat. No.: HY-W654009Loxoprofen-d3 is deuterium labeled Loxoprofen. Loxoprofen is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen can reduce atherosclerosis and shows antitumor activity.
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Trifenagrel (Standard)
0 ImagesCat. No.: HY-105872RCAS No.: 84203-09-8Trifenagrel (Standard) is the analytical standard of Trifenagrel (HY-105872). This product is intended for research and analytical applications. 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.
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Tenoxicam (Standard)
0 ImagesSynonyms: Ro-12-0068 (Standard)Tenoxicam (Standard) is the analytical standard of Tenoxicam. This product is intended for research and analytical applications. Tenoxicam (Ro-12-0068), an antiinflammatory agent with analgesic and antipyretic properties.
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Loxoprofen (Standard)
0 ImagesLoxoprofen (Standard) is the analytical standard of Loxoprofen. This product is intended for research and analytical applications. Loxoprofen is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen can reduce atherosclerosis and shows antitumor activity.
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Oxyphenbutazone (Standard)
0 ImagesCat. No.: HY-B1355ARCAS No.: 129-20-4Oxyphenbutazone (Standard) is the analytical standard of Oxyphenbutazone. This product is intended for research and analytical applications. Oxyphenbutazone is a Phenylbutazone (HY-B0230) metabolite, with anti-inflammatory effect. Oxyphenbutazone is an orally active non-selective COX inhibitor. Oxyphenbutazone selectively kills non-replicating Mycobaterium tuberculosis.
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Mavacoxib (Standard)
0 ImagesCat. No.: HY-119447RCAS No.: 170569-88-7Mavacoxib (Standard) is the analytical standard of Mavacoxib. This product is intended for research and analytical applications. Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs.
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Haloperidol decanoate (Standard)
0 ImagesCat. No.: HY-107969RCAS No.: 74050-97-8Haloperidol decanoate (Standard) is the analytical standard of Haloperidol decanoate. This product is intended for research and analytical applications. Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate can increase the striatal D2 receptor in rat. Haloperidol decanoate can improve conditions of psychoses (mainly schizophrenia). Haloperidol decanoate can lead to increased accumulation of the dopamine metabolites homo-vanillic acid. Haloperidol decanoate can reduce intestinal transport, increase gastric emptying and reduce acid output in rat model.
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Rebamipide mofetil (Standard)
0 ImagesCat. No.: HY-109158RCAS No.: 1527495-76-6Rebamipide mofetil (Standard) is the analytical standard of Rebamipide mofetil (HY-109158). This product is intended for research and analytical applications. 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.
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Tamarixetin (Standard)
0 ImagesTamarixetin (Standard) is the analytical standard of Tamarixetin. This product is intended for research and analytical applications. Tamarixetin (4'-O-Methyl Quercetin) is an orally active natural flavonoid derivative of quercetin and caseinolytic protease p (ClpP) inhibitor with anti-inflammatory, antioxidant and antitumor effects. Tamarixetin inhibits the hydrolytic activity of ClpP to the fluorescent substrate Suc-LY-AMC with an IC50 of 49.73 μM, which can be used for the study of Staphylococcus aureus infection. Tamarixetin inhibits tumor cell growth, induces apoptosis, and cell cycle arrest. Tamarixetin prevents cardiac hypertrophy by inhibiting the NFAT and AKT pathways.
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Nimesulide-13C6
0 ImagesCat. No.: HY-B0363S1Synonyms: R805-13C6
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Cimicoxib (Standard)
0 ImagesCat. No.: HY-100516RCAS No.: 265114-23-6Synonyms: UR-8880 (Standard)Cimicoxib (Standard) is the analytical standard of Cimicoxib. This product is intended for research and analytical applications. Cimicoxib (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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Sinapaldehyde (Standard)
0 ImagesSinapaldehyde is a methoxyphenol and a selective COX-2 inhibitor (IC50: 47.8 µM) that can be extracted from various plants. Sinapaldehyde has antibacterial, anti-inflammatory, and antioxidant activities. Sinapaldehyde can scavenge DPPH free radicals (IC50: 172 μM). Sinapaldehyde is active against both Gram-negative and Gram-positive bacteria.
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Piketoprofen (Standard)
0 ImagesPiketoprofen (Standard) is the analytical standard of Piketoprofen. This product is intended for research and analytical applications. Piketoprofen is a non-steroidal anti-inflammatory reagent that can be used as a cream preparation for the study of soft tissue rheumatism.
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EIPA hydrochloride (Standard)
0 ImagesSynonyms: L593754 hydrochloride (Standard); MH 12-43 hydrochloride (Standard); Ethylisopropylamiloride hydrochloride (Standard)EIPA (hydrochloride) (Standard) is the analytical standard of EIPA (hydrochloride). This product is intended for research and analytical applications. EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.
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(-)-Bornyl ferulate
0 ImagesCat. No.: HY-W706470CAS No.: 55511-07-4(-)-Bornyl ferulate is a 5-lipoxygenase and COX inhibitor with IC50s of 10.4 μM and 12.0 μM, respectively.
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Diclofenac diethylamine (Standard)
0 ImagesDiclofenac (diethylamine) (Standard) is the analytical standard of Diclofenac (diethylamine). This product is intended for research and analytical applications. 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.
