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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PPARγ agonist 19
0 ImagesCat. No.: HY-176214PPARγ agonist 19 (Compound 5e) is a PPARγ agonist. PPARγ agonist 19 has an IC50 of 11.27 μM against COX-1 and an IC50 of 0.05 μM against COX-1. PPARγ agonist 19 increases glucose uptake in rat hemidiaphragm assay and is superior to pioglitazone (HY-13956). PPARγ agonist 19 alleviates hyperglycemia and insulin resistance in an in vivo model of type 2 diabetes in rats and protects against renal and lipidemia damage caused by metabolic dysfunction.
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COX-2-IN-59
0 ImagesCat. No.: HY-179125COX-2-IN-59 is a potent and selective COX-2 inhibitor with an IC50 of 0.052 μM. COX-2-IN-59 exhibits 200-fold selectivity over COX-1 (IC50 = 11.16 μM). COX-2-IN-59 reduces COX-2 levels, induces cell cycle arrest, and triggers apoptosis by increasing Bax expression, decreasing Bcl-2 levels, and activating caspase-3. COX-2-IN-59 can be used for the research of colon cancer.
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XO/COX/LOX-IN-1
0 ImagesCat. No.: HY-151173CAS No.: 2831329-35-0XO/COX/LOX-IN-1 is a XO/COX/LOX inhibitor with an IC50 of 3.2 μM against rat XO, 10.83 μM against 5-LOX, 12.67 μM against COX-1, and 8.31 μM against COX-2. XO/COX/LOX-IN-1 binds to the active sites of XO, 5-LOX, COX-1 and COX-2, thereby blocking enzyme activities associated with uric acid, leukotriene, prostaglandin synthesis and inflammatory pathways. XO/COX/LOX-IN-1 can be used in the research of hyperuricemia and inflammation.
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ATP Synthesis-IN-4
0 ImagesCat. No.: HY-181602ATP Synthesis-IN-4 is a mitochondria-targeted small-molecule ligand that inhibits ATP synthesis. ATP Synthesis-IN-4 binds to mtDNA G4s in melanoma cells, thereby inducing changes in mitochondrial metabolism and inhibiting cell proliferation. ATP Synthesis-IN-4 suppresses the translation of key mitochondrial respiratory chain proteins (CYTB, ATP8, COX1, COX3, ND2) in melanoma cells, downregulates the expression of OXPHOS complexes, activates the phosphorylation of AMPK, and induces metabolic reprogramming to upregulate glycolysis. ATP Synthesis-IN-4 is applicable to relevant research on melanoma.
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Jusneesiinol
0 ImagesCat. No.: HY-N21710CAS No.: 216955-78-1Jusneesiinol is a lignan-class prostaglandin synthesis inhibitor and COX-1/COX-2 inhibitor that exerts central analgesic, peripheral analgesic, and antipyretic effects by inhibiting prostaglandin formation, antagonizing prostaglandin receptors, and inhibiting lipid peroxidation. Jusneesiinol can be used in research on pain and fever.
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15-LOX-IN-2
0 ImagesCat. No.: HY-17311515-LOX-IN-2 (Compound 2a) is an orally active COX-2/15-LOX inhibitor and a partial agonist of PPARγ. 15-LOX-IN-2 has anti-inflammatory activity and inhibits the levels of 20-HETE, IL-1β and TNF-α in RAW 264.7 cells treated with LPS (HY-D1056). In addition, 15-LOX-IN-2 has significant glucose uptake capacity in the absence of insulin. 15-LOX-IN-2 can be used for the research of metabolic diseases.
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COX-2-IN-61
0 ImagesCat. No.: HY-179700COX-2-IN-61 is an orally active COX-2 inhibitor with an IC50 of 22 µM, also inhibits COX-1 with an IC50 of 43 µM. COX-2-IN-61 exhibits anti-inflammation effects in a Carrageenan (HY-125474) induced rat paw edema model, with promising safety profiles. COX-2-IN-61 can be used for the research of inflammation.
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Dihydroflavokawin B
0 ImagesCat. No.: HY-W676872CAS No.: 3791-76-2Dihydroflavokawin B is a selective COX-1 inhibitor with an IC50 of 1.22 μM. Dihydroflavokawin B weakly inhibits COX-2 and 5-LOX. Dihydroflavokawin B inhibits promastigote forms of Leishmania panamensis and Leishmania braziliensis. Dihydroflavokawin B inhibits rabbit platelet aggregation induced by Arachidonic acid, platelet activating factor, and adenosine diphosphate. Dihydroflavokawin B exhibits in vitro anti-inflammatory activity. Dihydroflavokawin B can be used for the research of leishmaniasis.
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Triflusal-d3
0 ImagesCat. No.: HY-B0531SCAS No.: 2748541-63-9Triflusal-d3 is deuterium labeled Triflusal (HY-B0531). 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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Eltenac
0 ImagesCat. No.: HY-106093CAS No.: 72895-88-6Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood.
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Multi-kinase-IN-8
0 ImagesCat. No.: HY-179439Multi-kinase-IN-8 is a muti-kinase inhibitor. Multi-kinase-IN-8 inhibits COX-1 (IC50 of 12.6 μM), COX-2 (IC50 of 0.05 μM) and VEGFR-2 (IC50 of 0.12 nM). Multi-kinase-IN-8 inhibits tumor-associated carbonic anhydrases (CA IX and CA XII with Ki of 31.5 nM and 386.9 nM, respectively). Multi-kinase-IN-8 triggers cell cycle arrest and apoptosis through upregulation of Caspase 9 and Bax along with downregulation of Bcl 2. Multi-kinase-IN-8 suppresses PGE2, p-VEGFR-2, MMP-9 and HIF-1α and exhibits growth-inhibitory activity against breast cancer, lung cancer, and colorectal adenocarcinoma.
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COX-2/15-LOX-IN-7
0 ImagesCat. No.: HY-179021CAS No.: 1860810-23-6COX-2/15-LOX-IN-7 is a potent, selective and orally active dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.022 and 1.19 μM. COX-2/15-LOX-IN-7 also inhibits COX-1 with an IC50 value of 28.081μM. COX-2/15-LOX-IN-7 has low cytotoxicity against human colorectal cancer HT-29 and HCT116 cell lines (IC50 >100 μM for both). COX-2/15-LOX-IN-7 exhibits non-ulcerogenic performance. COX-2/15-LOX-IN-7 can be used for the research of cancer.
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Tomoxiprole
0 ImagesCat. No.: HY-105874CAS No.: 76145-76-1Synonyms: MDL 035Tomoxiprole (MDL 035) is a new analgesic antiinflammatory agent. Tomoxiprole selectively inhibits cyclooxygenase-2 (IC50 = 7 nM) .
