human cox-1

Diclofenac (Diclofenacum) is a nonsteroidal benzeneacetic acid derivative with anti-inflammatory activity. Diclofenac binds and chelates both isoforms of cyclooxygenase (COX-1 and-2), thereby blocking the conversion of arachidonic acid to pro-inflammatory-proprostaglandins.

Diclofenac Diethylamine, a non-selective COX inhibitor, is utilized as a nonsteroidal anti-inflammatory drug (NSAID).

Loxoprofen (Koloxo) is an anti-inflammatory non-steroidal medicine.

Piroxicam (CP-16171) is a non-specific COX inhibitor.

Mefenamic acid (CN-35355) is a non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.

Diclofenac sodium (GP 45840) is a non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.

Etoricoxib (MK-663) is a synthetic, nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic, and potential antineoplastic properties. Etoricoxib specifically binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in inhibition of the conversion of arachidonic acid into prostaglandins. Inhibition of COX-2 may induce apoptosis and inhibit tumor cell proliferation and angiogenesis.

2,6-Dichlorodiphenylamine, an analogue of Diclofenac Sodium, exhibits anti-Candida albicans activity. Diclofenac Sodium, a potent and nonselective COX inhibitor, has IC50 values of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells. [1]. Makoto Urai, et al. Potent Drugs That Attenuate anti-Candida albicans Activity of Fluconazole and Their Possible Mechanisms of Action. J Infect Chemother. 2014 Oct;20(10):612-5.

Diclofenac Potassium (CGP-45840B) is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions.

ML351 is a potent and selective inhibitor of human 15-lipoxygenase-1 (15 LOX)(IC50: 200 nM).

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2 iNOS expression.

1. Cornuside (Comuside) has immunomodulatory activity . 2. Cornuside suppresses expression levels of cytokine-induced proinflammatory and adhesion molecules in the human endothelial cells. 3. Cornuside can treat myocardial I R and protect the liver from CCl4-induced acute hepatotoxicity, by reducing oxidative stress and suppressing inflammatory responses. 4. Cornuside has anti-inflammatory activity by downregulations of iNOS and COX-2 due to NF-κB inhibition as well as the negative regulation of ERK1 2, p38, and JNK1 2 phosphorylations in RAW 264.7 cells. 5. Cornuside has protective potential against cerebral ischemic injury, may be due to the suppression of intracellular Ca(2+) elevation and caspase-3 activity, and improvements in mitochondrial energy metabolism and antioxidant properties.

DuP-697 is an irreversible, specific COX-2 inhibitor with IC50 values ​​of 10 nM and 800 nM for human COX-2 and COX-1. DuP-697 also exhibits anti-angiogenic, anti-inflammatory, antipyretic and apoptotic effects.

Nitroaspirin (NCX 4016) is a nitric oxide donor and a nitro-derivative of Aspirin that inhibits cyclooxygenase. It induces cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells by down-regulating EGFR PI3K STAT3 signaling and modulating Bcl-2 family proteins. Additionally, Nitroaspirin possesses antithrombotic and antiplatelet properties and acts as a direct and irreversible inhibitor of COX-1.

Indomethacin-D4 is a deuterium labeled Indomethacin. Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells.

Piroxicam D3 is deuterium labeled Piroxicam. Piroxicam is a COX inhibitor(human monocyte COX-1 and COX-2 with IC50s of 47, 25 μM , respectively) .

Acemetacin (TVX 1322) is a carboxymethyl ester of indometacin and a potent non-steroidal anti-inflammatory drug derived from indol-3-acetic acid, with its activity primarily attributed to its active metabolite, indomethacin. In clinical trials, acemetacin shows better gastric tolerability compared to indomethacin.

HQL-79 is a selective and orally active human hematopoietic prostaglandin D synthase (H-PGDS) inhibitor. It inhibits the synthesis of PGD2 and acts as an anti-allergic agent (Kd: 0.8 μM and IC50: 6 μM). It also shows no obvious effect on COX-1, COX-2, m-P

Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor (IC50: 18 nM) that also inhibits COX-1 activity (IC50: 115 nM) and exhibits anti-inflammatory effects.

AGU654 (Compound 44) is a selective mPGES-1 inhibitor with an IC50 value of 2.9 nM against mPGES-1. By inhibiting mPGES-1, AGU654 interrupts the pathway where COX-1 2 converts arachidonic acid to prostaglandin E2 (PGE2), effectively reducing inflammatory responses, pain, and fever symptoms. In models using activated human monocyte-derived macrophages and whole blood, AGU654 selectively inhibits PGE2 production induced by bacterial endotoxins, while preserving the production of other prostaglandins. In guinea pig models, AGU654 significantly alleviates fever, inflammation, and inflammatory pain, demonstrating excellent anti-inflammatory, analgesic, and antipyretic effects. AGU654 holds promise as a new approach for researching inflammatory diseases and pain.

FR 122047 (1-[(4,5-Bis(4-methoxyphenyl-2-thiazoyl)carbonyl]-4-methylpiperazine, Hydrochloride) is a potent and selective inhibitor of COX-1 with IC50 of 28 nM and 65 µM for human recombinant COX-1 and COX-2, respectively.

SC-58125 is a selective cyclooxygenase 2 (COX-2) inhibitor, with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo, and it also can inhibit edema at the inflammatory site and is analgesic

Cinnamtannin B-1 (LDN 0022358) is an A-type proanthocyanidin contained in several plant species such as Vaccinium vitis-idaea, Laurus nobilis L., Cinnamomum zeylanicum, and Lindera umbellata. It is a potent antioxidant and protective agent against oxidative stress and apoptosis in human platelets. It is a Cox-2 inhibitor.

Tolmetin (Tolectin) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of tolmetin is as a Cyclooxygenase Inhibitor. The chemical classification of tolmetin is Nonsteroidal Anti-inflammatory Compounds.