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]^[4]. 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]^[4]^[5]. 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]^[4]^[5]. 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]^[5].

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]

COX-1 Related Products (190):

By Type:	Pan (112) Selective (48)
By Effects:	Inhibitors (189) Control (1)

Cat. No.	Product Name	Effect	Purity

HY-B1130R

Isoxicam (Standard)	Inhibitor
Isoxicam (Standard) is the analytical standard of Isoxicam (HY-B1130). This product is intended for research and analytical applications. Isoxicam is an orally active nonsteroidal anti-inflammatory compound and a COX-1/COX-2 inhibitor. Isoxicam exhibits potent anti-inflammatory activity in rat models of inflammation and significantly lower ulcerogenic risk. Isoxicam can be used for the study of inflammatory diseases and rheumatic disorders.

HY-W744923

Bis[2-(4-hydroxyphenylthio)ethoxy]methane	Inhibitor	99.59%
Bis[2-(4-hydroxyphenylthio) ethoxy]methane (DD-70) is a Bisphenol A (HY-18260) substitute and a COX-1 inhibitor. Bis[2-(4-hydroxyphenylthio) ethoxy]methane blocks platelet aggregation induced by Arachidonic acid (HY-109590) and U-46619 (HY-108566). Bis[2-(4-hydroxyphenylthio) ethoxy]methane alters hemostatic function. Bis[2-(4-hydroxyphenylthio) ethoxy]methane reduces embryonic survival rate, decreases embryonic mass and increases gallbladder mass in chicken embryos.

HY-B0227A

Ketoprofen (lysinate)	Inhibitor
Ketoprofen (RP-19583) lysinate is a non-steroidal anti-inflammatory agent. Ketoprofen lysinate can inhibit the activity of cyclooxygenase with IC₅₀ values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity.

HY-14654A

Aspirin lithium	Inhibitor
Aspirin (Acetylsalicylic Acid) lithium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin lithium induces apoptosis. Aspirin lithium inhibits the activation of NF-κB. Aspirin lithium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.

HY-15034

Indomethacin sodium	Inhibitor
Indomethacin (Indometacin) sodium is a potent, orally active COX1/2 inhibitor with IC₅₀ values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin sodium has anticancer activity and anti-infective activity. Indomethacin sodium can be used for cancer, inflammation and viral infection research..

HY-150553

COX-2-IN-28	Inhibitor
COX-2-IN-28 is a potent and selective COX-2 inhibitor with IC₅₀ values of 0.054, 2.14, 13.21 µM for COX-2, 15-LOX, COX-1,respectively.

HY-B1799A

Tolmetin sodium	Inhibitor
Tolmetin sodium is an orally active and potent COX inhibitor with IC₅₀s of 0.35 μM and 0.82 μM human COX-1 and COX-2, respectively. Tolmetin sodium is a non-steroidal anti-inflammatory drug (NSAID).

HY-108019

SD 8381	Inhibitor
SD 8381 is a potent and selective COX-2 inhibitor. SD 8381 shows IC₅₀ values of 0.0098 μM for hCOX-2 and 0.69 μM for hCOX-1.

HY-122953

Daturaolone	Inhibitor
Daturaolone is a natural triterpenoid with anti-inflammatory and antinociceptive potentials. Daturaolone displays a COX-1 inhibitory activity.

HY-162167

COX-1-IN-1	Inhibitor
COX-1-IN-1 (compound 15a) is a selective inhibitor for cyclooxygenase (COX), with IC₅₀s of 0.23 μM (COX-1) and >50 μM (COX-2), selective index (COX-2 IC₅₀/COX-1 IC₅₀) is 217. COX-1-IN-1 inhibits platelet aggregation.

HY-115967

COX-1/2-IN-2	Inhibitor
COX-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 9.7 ± 0.09 µM and 4.6 ± 1.45 µM, respectively.

HY-121828

TX-1123	Inhibitor
TX-1123 is a potent protein tyrosine kinase (PTK) inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC. TX-1123 is a cyclo-oxygenase (COX) inhibitor with IC₅₀ values of 1.16 μM and 15.7 μM for COX2 and COX1, respectively. TX-1123 has low mitochondrial toxicity. TX-1123 can be used in research of cancer.

HY-147815

COX-2-IN-21	Inhibitor
COX-2-IN-21 (Compound 5c) is a selective and orally active COX-2 inhibitor with an IC₅₀ of 0.039 μM. COX-2-IN-21 shows promising anti-inflammatory potential.

HY-150551

COX-2-IN-27	Inhibitor
COX-2-IN-27 is a potent and selective COX-2 inhibitor with IC₅₀ values of 13.22, 0.045, 1.67 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-27 shows anti-inflammatory activity.

HY-123639

LM-4108	Inhibitor
LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC₅₀ of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively.

HY-147748

COX-2-IN-17	Inhibitor
COX-2-IN-17 (compound 10) is a potent and BBB-penetrated COX-2 (cyclooxygenase-2) inhibitor, with an IC₅₀ of 0.02 μM. COX-2-IN-17 shows anti-inflammatory and analgesic activities. COX-2-IN-17 attenuates hyperalgesia in the neurogenic phase as well as the inflammatory phase.

HY-N15530

2,5-Dimethoxy-3-glucopyranosylcinnamic alcohol	Inhibitor
2,5-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 .

HY-N9765

threo-Guaiacylglycerol β-coniferyl ether	Control
threo-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).

HY-W032938

COX-1-IN-4	Inhibitor
COX-1-IN-4 (Compound P10) is a selective COX-1 inhibitor (IC₅₀s: COX-1 = 0.09 μM; COX-2 = 2.49 μM). COX-1-IN-4 reduces the production of NO as well as the expression of the iNOS protein. COX-1-IN-4 can be used in the research of neuroinflammation.

HY-159634

Zidometacin	Inhibitor
Zidometacin 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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