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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Pifoxime
0 ImagesCat. No.: HY-148224CAS No.: 31224-92-7Pifoxime is a COX-1/2 inhibitor, a non-steroidal anti-inflammatory agent (NSAID). Pifoxime shows anti-inflammatory activity, and can be used in neuropsychiatric research.
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Loxoprofen sodium dihydrate
0 ImagesCat. No.: HY-B0578BCAS No.: 226721-96-6Loxoprofen sodium dihydrate is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium dihydrate is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium dihydrate can reduce atherosclerosis and shows antitumor activity.
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7-Methoxy-4H-chromen-4-one-o-carborane
0 ImagesCat. No.: HY-183188CAS No.: 3097646-97-1
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COX-1-IN-5
0 ImagesCat. No.: HY-160184CAS No.: 524699-85-2COX-1-IN-5 (example 13, compound PS13) is a potent and selective COX-1 inhibitor (COX-1 IC50 = 1 nM, COX-2 IC50 > 0.1 μM) exhibiting >1000-fold selectivity over COX-2. COX-1-IN-5 possesses strong anti-inflammatory, antipyretic, analgesic, antithrombotic, anti-cancer activities. COX-1-IN-5 can be used for COX-mediated diseases research, such as inflammatory conditions and pain. COX-1-IN-5 radiolabeled with 11C can be used as a selective PET tracer for whole‑body imaging of COX‑1 distribution and target engagement in vivo.
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COX-2-IN-19
0 ImagesCat. No.: HY-146198CAS No.: 2497530-12-6COX-2-IN-19 (Compound 24) is a potent COX-2 inhibitor with an IC50 of 1.76 μM. COX-2-IN-19 shows in vivo anti-inflammatory activity.
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COX-2-IN-52
0 ImagesCat. No.: HY-168888COX-2-IN-52 (Compound 5l) is an orally active and selective COX-2 inhibitor with an IC50 of 54 nM. COX-2-IN-52 can inhibit the release of NO in cells and has anti-inflammatory activity. COX-2-IN-52 has high gastrointestinal safety and can be used in the research of oral anti-inflammatory drugs.
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COX-2-IN-66
0 ImagesCat. No.: HY-183288COX-2-IN-66 is a cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 8.43 μM. COX-2-IN-66 reduces release of pro-inflammatory cytokines IL-6 and TNF-α. COX-2-IN-66 exhibits acceptable cellular tolerability, with cytokine-modulating concentrations remaining below its cytotoxic threshold. COX-2-IN-66 can be used for the research of inflammation.
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COX-2-IN-29
0 ImagesCat. No.: HY-150721CAS No.: 3033545-21-7COX-2-IN-29 (Compound 15b) is a selective and orally active COX-2 inhibitor with an IC50 of 0.005 μM.
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Mefenamic acid-d4
0 ImagesMefenamic acid-d4 is a deuterium labeled Mefenamic acid. Mefenamic acid is a BBB-permeable non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
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COX/5-LO-IN-2
0 ImagesCat. No.: HY-181061COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC50 of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast cancer.
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(±)-Aiphanol
0 ImagesCat. No.: HY-152120CAS No.: 578020-29-8Synonyms: Aiphanol(±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak.(±)-Aiphanol effectively inhibits VEGFR2 (IC50=0.92 μM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active.
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COX-2-IN-71
0 ImagesCat. No.: HY-189395COX-2-IN-71 is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.18 μM, and shows relatively weak inhibitory activity against COX-1 with an IC50 of 65.0 μM. COX-2-IN-71 is predicted to possess favorable drug-likeness, high gastrointestinal absorption, and compliance with Lipinski's rule of five. COX-2-IN-71 can be used for research on inflammatory diseases.
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CXT29
0 ImagesCat. No.: HY-179246CXT29 is an orally active COX-2 inhibitor and a thromboxane A2 receptor (TP) antagonist. CXT29 exhibits COX inhibitory activity and selectivity, with IC50 values of 13 and 722 nM for COX-2 and COX-1 respectively. CXT29 inhibits platelet aggregation induced by U-46619 (HY-108566) (a TP agonist), with an IC50 of 96 nM. CXT29 effectively inhibits the production of TXB₂ and PGE₂, significantly reducing platelet aggregation and inflammatory pain in mice. CXT29 can be used for research on inflammatory pain and cardiovascular diseases.
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COX-2-IN-20
0 ImagesCat. No.: HY-147809CAS No.: 2529451-43-0COX-2-IN-20 (Compound 5d) is a selective and orally active COX-2 inhibitor with an IC50 of 17.9 nM. COX-2-IN-20 shows anti-inflammatory activity.
