human cox-2

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.

Tilmacoxib is a highly selective, time-dependent, and irreversible inhibitor of human COX-2 ( IC50: 85 nM in an enzyme assay).

LM-1685 is a potent and selective inhibitor of COX-2 IN human monocytes and whole blood with IC50 of 0.65µM and IC50 = 4.3μM, respectively, and is a potential compound for the treatment of inflammation.

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.

Triflusal (UR1501) is a 2-acetoxy-4-trifluoromethylbenzoic acid and it is an aspirin chemically-related molecule but not a derivative.

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.

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.

Melatonin D5, a deuterium-labeled version of melatonin, is a hormone produced by the pineal gland, known for its role as a selective ATF-6 inhibitor that promotes apoptosis in human hepatoma cells via COX-2 downregulation. Additionally, it activates melatonin receptors and exhibits antioxidative and anti-inflammatory properties.

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) .

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.

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

COX-2-IN-48 (5-25) serves as an inhibitor of COX-2, exhibiting an IC50 of 51.7 nM against human COX-2. It displays anti-inflammatory and analgesic effects in various rodent models through inhibition of the NF-κB pathway. COX-2-IN-48 (5-25) inhibits the degradation of IκB, phosphorylation and nuclear translocation of NF-κB p65, and the expression of COX-2 and iNOS.

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.

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

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