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].
References:
- [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 Related Products (740)
Related Products (740)
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Phellodendrine chloride (Standard)
0 ImagesCat. No.: HY-N0735RCAS No.: 104112-82-5Phellodendrine chloride (Standard) is the analytical standard of Phellodendrine chloride (HY-N0735). Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.
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COX-2/15-LOX-IN-3
0 ImagesCat. No.: HY-155160CAS No.: 3052736-47-4COX-2/15-LOX-IN-3 (compound 5k) is a dual inhibitor of COX-2/15-LOX with IC50s of 0.075 μM and 1.97 μM, respectively. COX-2/15-LOX-IN-3 can inhibit LPS-induced cell production of promoting cytokines (IL-6, ROS, and NO), with specific anti-inflammatory activity.
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4-Methylamino antipyrine-d3 hydrochloride
0 ImagesCat. No.: HY-135731AS4-Methylamino antipyrine-d3 (hydrochloride) is deuterium labeled 4-Methylamino antipyrine (hydrochloride). 4-Methylamino antipyrine hydrochloride is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic agent and can be used for pain and fever. 4-Methylamino antipyrine hydrochloride has analgesic, antipyretic, and relatively weak antiinflammatory properties.
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Glucametacine
0 ImagesCat. No.: HY-111392CAS No.: 52443-21-7Glucametacine is an anti-inflammatory agent.
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Oxaprozin-d10
0 ImagesCat. No.: HY-W709448Synonyms: Oxaprozinum-d10; Wy21743-d10Oxaprozin-d10 (Oxaprozinum-d10; Wy21743-d10) is the deuterium labeled Oxaprozin (HY-B0808). Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.
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Esculentic acid
0 ImagesCat. No.: HY-N3866CAS No.: 103974-74-9Esculentic acid is a selective COX-2 inhibitor and has anti-inflammatory effect. Esculentic acid is a pentacyclic triterpenoid that can be extracted from the Chinese herb Phytolacca esculenta.
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Sinapyl alcohol (Standard)
0 ImagesCat. No.: HY-W109812RCAS No.: 537-33-7Sinapyl alcohol (Standard) is the analytical standard of Sinapyl alcohol. This product is intended for research and analytical applications. Sinapyl alcohol is an orally active anti-inflammatory and antinociceptive agent. Sinapyl alcohol reduces the expression level of inducible NO synthase and COX-2[1].
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Ibufenac-13C6
0 ImagesCat. No.: HY-W756637Synonyms: Dytransin-13C6Ibufenac-13C6 (Dytransin-13C6) is the 13C-labeled Ibufenac (HY-W040672). Ibufenac (Dytransin) is an orally active nonsteroidal anti-inflammatory agent. Ibufenac exerts anti-inflammatory, analgesic and antipyretic effects. Ibufenac is being studied for the treatment of rheumatic diseases such as rheumatoid arthritis.
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SC-75416
0 ImagesCat. No.: HY-19500CAS No.: 215122-74-0SC-75416 is a selective cyclooxygenase-2 inhibitor. Its pharmacokinetic/pharmacodynamic (PK/PD) model was used for development and clinical trial simulation to design a study protocol to verify its analgesic effect in a post-oral surgery pain model. The simulation results showed that 360 mg of SC-75416 may provide better pain relief than 400 mg of ibuprofen. The actual clinical trial results confirmed this hypothesis, and 360 mg of SC-75416 was indeed superior to 400 mg of ibuprofen in pain relief. The PK/PD model of SC-75416 showed good predictive performance and successfully predicted its clinical effect. These research results show that SC-75416, as a new selective COX-2 inhibitor, has potential clinical application value in the management of post-oral surgery pain.
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(S)-(+)-Ketoprofen-13C,d3
0 ImagesCat. No.: HY-W778002CAS No.: 1330260-99-5(S)-(+)-Ketoprofen-13C,d3 is the deuterium and 13C-labeled S-(+)-Ketoprofen (HY-B2137). S-(+)-Ketoprofen is a potent inhibitor of both COX-1 and COX-2 with IC50s of 1.9 and 27 nM, respectively.
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Diclofenac Amide-13C6
0 ImagesCat. No.: HY-W747879Diclofenac Amide-13C6 is the 13C-labeled Diclofenac amide (HY-134521). Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg).
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Anti-inflammatory agent 68
0 ImagesCat. No.: HY-163117Anti-inflammatory agent 68 (compound 7b) is a dual inhibitor of carbonic anhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), with anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 68 has IC50s of 12.6 μM and 60 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 68 binding to different isoforms of carbonic anhydrase are 52.6 nM (CA I), 79.1 nM (CA II), 58.1 nM (CA IX), and 17.2 nM (CA XII).
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Neokadsuranic acid B
0 ImagesCat. No.: HY-N19877CAS No.: 123828-59-1Neokadsuranic acid B is a 14 (13→12)-seco-lanostane-type triterpenoid acid that exists in the stems of Kadsura longipedunculata and Radix Aconiti Lateralis Preparata. It has high binding affinity for PTGS2 (COX-2). Neokadsuranic acid B shows promise for research into rheumatoid arthritis.
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4'-Aarboxylic acid imrecoxib-d7
0 ImagesCat. No.: HY-144463S4'-Aarboxylic acid imrecoxib-d7 is the deuterium labeled 4'-Aarboxylic acid imrecoxib (HY-154846). 4'-Aarboxylic acid imrecoxib is a metabolite of Imrecoxib, a selective COX-II inhibitor.
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C2 Ceramide (d14:1/2:0)
0 ImagesCat. No.: HY-116877CAS No.: 2097561-20-9C2 Ceramide (d14:1/2:0) is a composition for diagnosing diseases associated with cyclooxygenase 2 (COX2) overexpression. C2 Ceramide (d14:1/2:0) exhibits a strong binding activity to COX2 protein (extracted from patent WO2019235824A1).
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Macelignan (Standard)
0 ImagesCat. No.: HY-N0064RCAS No.: 107534-93-0Synonyms: (+)-Anwulignan (Standard); Anwuligan (Standard)Macelignan (Standard) is the analytical standard of Macelignan. This product is intended for research and analytical applications. Macelignan ((+)-Anwulignan; Anwuligan) is an orally active lignan isolated from Myristica fragrans. Macelignan possesses many pharmacological activities, including anti-inflammatory, anti-cancer, anti-diabetes, and neuroprotective activities.
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Lonazolac hemicalcium
0 ImagesCat. No.: HY-137149CAS No.: 75821-71-5Lonazolac (hemicalcium) is the calcium salt form of Lonazolac. Lonazolac is a nonsteroidal antirheumatic agent with anti-inflammatory properties.
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Deracoxib (Standard)
0 ImagesSynonyms: SC 046 (Standard); SC 46 (Standard); SC 59046 (Standard)Deracoxib (SC 046; SC 59046) (Standard) is the analytical standard of Deracoxib (HY-17509). This product is intended for research and analytical applications. Deracoxib, an orally active COX-2 inhibitor, is a veterinary nonsteroidal anti-inflammatory agent used exclusively in dogs. Deracoxib inhibits the COX-2 enzyme to reduce the production of prostaglandins, effectively controlling pain and inflammation after canine soft tissue surgery. Deracoxib reduces the inhibition of COX-1 and lowers the risk of gastrointestinal side effects. Deracoxib induces tumor cell cycle arrest and apoptosis, and shows anti-tumor activity in canine osteosarcoma, breast tumors and bladder transitional cell carcinomas
