COX-1
COX-1 (cyclooxygenase-1, PTGS1) is a constitutively expressed prostaglandin-endoperoxide synthase that catalyzes the conversion of arachidonic acid into prostaglandin intermediates, thereby initiating prostaglandin and thromboxane biosynthesis essential for physiological homeostasis[1][2]. Mechanistically, COX-1 participates in the cyclooxygenase and peroxidase reactions that generate prostaglandin H2, a central precursor for multiple bioactive prostanoids regulating vascular function, platelet activity, renal perfusion, and gastrointestinal integrity[1][3]. Through sustained prostanoid production, COX-1 contributes to tissue-protective and housekeeping functions across mammalian organs, including maintenance of gastric mucosal defense and thromboxane A2-dependent platelet aggregation[3][2]. In disease and pharmacological models, inhibition of COX-1 reduces prostaglandin synthesis and underlies the therapeutic actions of aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs), while also contributing to gastrointestinal adverse effects associated with nonselective COX blockade[1][2][4]. Compared with the inducible isoform COX-2, which is preferentially upregulated by inflammatory stimuli and cellular stress, COX-1 exhibits stable basal expression and is primarily associated with physiological regulation rather than acute inflammatory responses[3][2][4]. For experimental applications, selective and nonselective COX inhibitors remain important tools for dissecting prostanoid-dependent signaling pathways and distinguishing constitutive versus inducible cyclooxygenase functions in inflammation, thrombosis, and tissue homeostasis[1][3][4].
References:
- [1]. Fitzpatrick FA. Cyclooxygenase enzymes: regulation and function. Curr Pharm Des. 2004;10(6):577-88. doi: 10.2174/1381612043453144. PMID: 14965321. et al. Cyclooxygenase enzymes: regulation and function. Curr Pharm Des. 2004;10(6):577-88. [Content Brief]
- [2]. Database: Guide to pharmacology.
- [3]. Vane JR, et al. Cyclooxygenases 1 and 2. Annu Rev Pharmacol Toxicol. 1998;38:97-120. [Content Brief]
- [4]. Database: Guide to pharmacology.
- [5]. Rouzer CA, et al. Structural and Chemical Biology of the Interaction of Cyclooxygenase with Substrates and Non-Steroidal Anti-Inflammatory Drugs. Chem Rev. 2020 Aug 12;120(15):7592-7641. [Content Brief]
All Product Categories
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COX-1 Related Products (200)
Related Products (200)
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2,5-Dimethoxy-3-glucopyranosylcinnamic alcohol
0 ImagesCat. No.: HY-N15530CAS No.: 251660-72-72,5-Dimethoxy-3-glucopyranosylcinnamic alcohol is found in P. crocatum and Dirca palustris. 2,5-Dimethoxy-3-glucopyranosylcinnamic alcohol is a COX-I inhibitor. 2,5-Dimethoxy-3-glucopyranosylcinnamic alcohol has anti-inflammatory activity .
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threo-Guaiacylglycerol β-coniferyl ether
0 ImagesCat. No.: HY-N9765CAS No.: 168393-18-8threo-Guaiacylglycerol β-coniferyl ether (compound 9) is a potentially active compound, but its inhibitory activity against NF-κB, nitric oxide production, aromatase, quinone reductase 2, and cyclooxygenase (COX-1/-2) is not significant. threo-Guaiacylglycerol β-coniferyl ether can be naturally extracted from the 95% ethanol extract of the whole plant of Lepisorus contortus (Christ) Ching (a plant of the Polypodiaceae family).
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Zidometacin
0 ImagesCat. No.: HY-159634CAS No.: 62851-43-8Zidometacin is a nonsteroidal anti-inflammatory agent. Zidometacin significantly inhibits prostaglandin synthesis with low gastrolesive influence. Zidometacin has antinociceptive and antipyretic activities and shows relatively low ulcerogenicity in rat models. Zidometacin can be used for analgesia and osteoarthritis research.
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COX-1/2-IN-1
0 ImagesCat. No.: HY-115966CAS No.: 2358849-47-3COX-1/2-IN-2 is a potent COX1/2 inhibitor. COX-1/2-IN-2 exhibits significant inhibitory effect against COX-1 and COX-2 inhibitor with IC50 values of 13.9 ± 3.21 µM and 6.4±0.74 µM, respectively.
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COX-2-IN-31
0 ImagesCat. No.: HY-149270CAS No.: 3039955-76-2
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D-Glycero-D-galacto-heptose
0 ImagesCat. No.: HY-W854474CAS No.: 5328-64-3D-glycero-D-galacto-heptose is a seven-carbon sugar that exerts immunomodulatory effects. It is the structural monosaccharide unit of the Eubacterium saburreum T18 antigen, enhances immune cell activation, and acts as a COX-2 ligand to participate in anti-inflammatory pathways. D-glycero-D-galacto-heptose can be used in research on triple-negative breast cancer.
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COX-2/sEH-IN-1
0 ImagesCat. No.: HY-146704CAS No.: 2474977-38-1COX-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.
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COX-2-IN-60
0 ImagesCat. No.: HY-179142CAS No.: 3073624-74-2COX-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.
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COX-2-IN-30
0 ImagesCat. No.: HY-149269CAS No.: 1160498-08-7COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect.
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cis-5-Dodecenoic acid (Standard)
0 Imagescis-5-Dodecenoic acid (Standard) is the analytical standard of cis-5-Dodecenoic acid (HY-N8469). This product is intended for research and analytical applications. cis-5-Dodecenoic acid is an inhibitor of COX-I and COX-II with anti-inflammatory activity. cis-5-Dodecenoic acid reduces prostaglandin synthesis by inhibiting COX enzyme activity and is involved in the fatty acid -β oxidative metabolic pathway. The metabolic rate of cis-5-Dodecenoic acid is significantly lower than that of saturated fatty acids. cis-5-Dodecenoic acid can be used in the research of anti-inflammation, fatty acid metabolism mechanisms and related physiological and pathological processes.
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Oxaprozin potassium
0 ImagesCat. No.: HY-B0808ACAS No.: 174064-08-5Synonyms: Oxaprozinum potassium; Wy21743 potassiumOxaprozin potassium 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 potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.
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EGFR/COX-2-IN-1
0 ImagesCat. No.: HY-170932EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFRWT, EGFRT790M, COX-1 and COX-2 with IC50s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC50s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC50s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects.
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COX-2/CA II-1
0 ImagesCat. No.: HY-184937COX-2/CA II-1 is an orally active dual selective inhibitor targeting COX-2 and hCA II. COX-2/CA II-1 inhibits COX-2 with an IC50 value of 0.13 μM (SI = 9.25 vs COX-1) and hCA II with a Ki value of 39.1 nM (SI = 933.8 vs hCA I). COX-2/CA II-1 demonstrates significant analgesic and anti-inflammatory effects in animal models, shows improved gastric safety with reduced ulcerogenic liability, and exhibits intraocular pressure (IOP)-lowering effects in rabbit glaucoma models. COX-2/CA II-1 can be used for anti-inflammatory, analgesic and antiglaucoma research.
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COX-1/2-IN-3
0 ImagesCat. No.: HY-147693CAS No.: 2428387-82-8
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Parsalmide
0 ImagesCat. No.: HY-127145CAS No.: 30653-83-9
