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 (196)
Related Products (196)
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COX-2-IN-57
0 ImagesCat. No.: HY-175637COX-2-IN-57 is an orally active COX-2 inhibitor with an IC50 value of 0.02 μM. COX-2-IN-57 reduces MyD88 expression and decreases serum levels of COX-2, PGE2, and COX-1 in Cisplatin (HY-17394)/radiation-induced neuropathy rat model. COX-2-IN-57 demonstrates superior antinociceptive efficacy in hot plate, cold allodynia, and Randall-Selitto tests, along with hepato-/renal protection. COX-2-IN-57 can be used for the study of inflammation.
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4-Methoxycinnamic acid ethyl ester
0 Images4-Methoxycinnamic acid ethyl ester (Ethyl p-methoxycinnamate) is an orally active natural compound found. 4-Methoxycinnamic acid ethyl ester exerts anti-inflammatory effects by inhibiting cyclooxygenase (COX-1 (IC50 = 1.12 μM) and COX-2 (IC50 = 0.83 μM)), NF-κB (IC50 = 88.7 μM) and cytokine production (TNF-α (IC50 = 96.84 μg/mL) and IL-1β (IC50 = 166.4 μg/mL)). 4-Methoxycinnamic acid ethyl ester inhibits tumor cell proliferation, migration and cancer metabolism and induces apoptosis.4-Methoxycinnamic acid ethyl ester inhibits VEGF expression, thereby inhibiting angiogenesis. 4-Methoxycinnamic acid ethyl ester has a significant inhibitory effect on dengue virus and Mycobacterium tuberculosis. 4-Methoxycinnamic acid ethyl ester has analgesic effects in rats.
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Triflusal (Standard)
0 ImagesTriflusal (Standard) is the analytical standard of Triflusal (HY-B0531). This product is intended for research and analytical applications. Triflusal is an orally bioavailable, blood-brain barrier-permeable dual Cyclooxygenase-1 (COX-1)/cAMP phosphodiesterase inhibitor. Triflusal inhibits platelet aggregation, NF-κB activation, iNOS activity, and prostaglandin synthesis in ischaemic tissue. Triflusal stimulates neutrophil nitric oxide production, eNOS protein expression, and cNOS activity. Triflusal alleviates cerebral ischemic injury in rats and ameliorates pathological lesions and related gene expression in transgenic Alzheimer’s disease models. Triflusal can be used for the research of thromboembolic/ischemic cardiovascular and cerebrovascular diseases, and Alzheimer’s disease.
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NCX 466
0 ImagesCat. No.: HY-103388CAS No.: 1262956-64-8NCX 466 is an orally active COX-1 and COX-2 inhibitor that exhibits anti-inflammatory and analgesic effects. Additionally, NCX 466 acts as a NO donor, exerting anti-inflammatory and antioxidant effects by improving microcirculation. NCX 466 significantly reduces the levels of transforming growth factor-β (TGF-β) and oxidative stress markers (such as thiobarbituric acid reactive substances (TBARS) and 8-hydroxy-2'-deoxyguanosine (8-OHdG)), and it decreases leukocyte recruitment during inflammation by reducing myeloperoxidase (MPO) activity, thereby preventing bleomycin (HY-108345)-induced pulmonary fibrosis in mice.
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Indomethacin N-octyl amide
0 ImagesCat. No.: HY-134138CAS No.: 282728-65-8
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BF389
0 ImagesCat. No.: HY-106897CAS No.: 127245-22-1Synonyms: Biofor 389
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COX-1/2-IN-9
0 ImagesCat. No.: HY-162761COX-1/2-IN-9 (Compound 3n) is a potent and selective inhibitor of COX-1/2, with IC50 values of 0.031 µM and 0.01 µM, respectively. COX-1/2-IN-9 possesses both antibacterial and anti-inflammatory activities, effectively inhibiting MRSA 1478 (MIC=50 μg/mL) and multidrug-resistant S. lentus (MIC=50 μg/mL). COX-1/2-IN-9 holds significant potential to alleviate MRSA-induced pneumonia in immunocompromised states.
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Neosakuranin
0 ImagesCat. No.: HY-N17699CAS No.: 31187-54-9Neosakuranin is a flavonoid. Neosakuranin can be isolated from Sorbus commixta and the bark of P. cerasus. Neosakuranin exhibits suppressive effects on xanthine oxidase with an IC50 of 157.8 μM. Neosakuranin inhibits COX-l. Neosakuranin can be used in the research of inflammatory diseases.
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Tenidap sodium
0 ImagesCat. No.: HY-105028ACAS No.: 119784-94-0Synonyms: CP-66248 sodium
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Methosulide
0 ImagesCat. No.: HY-W792524CAS No.: 51765-76-5Methosulide (Compound 1d) is a selective COX-2 inhibitor with an IC50 value of 2.31 μM. Methosulide can be used in the research of inflammatory diseases.
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SARS-CoV-2 Mpro-IN-41
0 ImagesCat. No.: HY-173485SARS-CoV-2 Mpro-IN-41 (Compound 7e) is an orally active inhibitor of COX-2 and SARS-CoV-2 M pro (IC50 values are 9.66 μM and 13.24 μM, respectively). SARS-CoV-2 Mpro-IN-41 also has a certain inhibitory activity against COX-1 (IC50: 46.11 μM). SARS-CoV-2 Mpro-IN-41 can significantly inhibit the expression of inflammatory-related cytokines (such as TNF-α, IL-6, IL-1β) and exert anti-inflammatory effects. SARS-CoV-2 Mpro-IN-41 exerts anti-inflammatory and antiviral effects by selectively inhibiting COX-2 and SARS-CoV-2 M pro. SARS-CoV-2 Mpro-IN-41 can be used for anti-inflammatory and anti-coronavirus research.
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Catechin hydrate
0 ImagesCat. No.: HY-N0932CAS No.: 88191-48-4Synonyms: (+)-Catechin hydrate; Cianidanol hydrate; Catechuic acid hydrateCatechin hydrate inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM.
