COX

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

Esflurbiprofen is an inhibitor of COX-1 and COX-2.

2,5-Di-tert-butylhydroquinone (BHQ) is an effective and selective endoplasmic reticulum Ca2+-ATPase inhibitor.

Glafenine (Glafenin), a non-narcotic analgesic agent, is a non-steroidal anti-inflammatory drug (NSAID), and widely used for the therapy of pains of various origins.

Guaiacol (2-Methoxyphenol) is a precursor to various flavorants, such as eugenol and vanillin. Its derivatives are used medicinally as an expectorant, antiseptic, and local anesthetic. It also can be used as an indicator in chemical reactions that produce oxygen. When oxygen binds to it, the complex turns yellowish brown and absorbs light maximally at about 470 nm.

Ketorolac (Acuvail) is a non-steroidal anti-inflammatory drug (NSAID) in the family of heterocyclic acetic acid derivatives. It acts by inhibiting the bodily synthesis of prostaglandins.

(±)-Catechin ((±)-Catechin hydrate) hydrate is a natural product,has antioxidant activity and is effective in reducing oxidative stress.

4-Nonylphenol polyethoxylate (Nonoxinol-9) is a typical surfactant used as a vaginal spermicide. Spermicides are locally acting non-hormonal contraceptives. When present in the vagina during intercourse, they immobilize/inactivate/damage and/or kill sperms without eliciting systemic effects. 4-Nonylphenol polyethoxylate has been in use for more than 30 years as an over-the-counter (OTC) drug in creams, gels, foams and condom lubricants. It is the most commonly used spermicidal contraceptive in the UK and the USA. In several European countries, spermicides are no longer on the market.

Revaprazan hydrochloride (YH1885) is the hydrochloride salt form of a lipophilic, weak base with potassium-competitive acid blocking (P-CAB) activity.

Lornoxicam (Chlortenoxicam) (chlortenoxicam) is a new nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class with analgesic, anti-inflammatory, and antipyretic properties. Lornoxicam differs from other oxicam compounds in its potent inhibition of prostaglandin biosynthesis, a property that explains the particularly pronounced efficacy of the drug. Lornoxicam is approved for use in Japan.

Tenoxicam (Tilcotil), an antiinflammatory agent with analgesic and antipyretic properties, is used to treat osteoarthritis and control acute pain.

Paradol ([6]-Gingerone) is a pungent phenolic substance found in ginger and other Zingiberaceae plants, and exhibits a variety of biological activities including anti-cancer, anti-inflammatory, and anti-oxidative activities,neuroprotective Effects.

(R)-Naproxen, an anti-inflammatory agent, has antipyretic and analgesic properties. Both the acid and its sodium salt are used in the therapy of acute gout or dysmenorrhea, musculoskeletal disorders, rheumatoid arthritis and other rheumatic.

5-Aminosalicylic Acid (5-ASA) is an anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE.

Chlorotrianisene (tri-p-anisylchloroethylene) is an orally bioavailable, highly lipophilic, synthetic triphenylethylene (TPE) derivative and selective estrogen receptor modulator (SERM), with predominantly estrogenic but also antiestrogenic activities.

Gallic acid (Benzoic acid) is found in almost all plants. Plants known for their high gallic acid content include gallnuts,grapes,tea,hops and oak bark.

(-)-Epicatechin gallate ((-)-Epicatechin 3-O-gallate) is one of the catechin isomers and a potent antioxidant that can modulate a wide range of membrane proteins. Its bilayer-modifying potency was tested using gramicidin A (gA) channels as probes. All the catechins alter gA channel function and modify bilayer properties, with a 500-fold range in potency. The gallate group causes current block, as evident by brief downward current transitions.

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.

(-)-Epicatechin (Epicatechin) is an inhibitor of cyclooxygenase-1 (COX-1), inhibiting the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Indomethacin (Indometacin) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of indomethacin is as a Cyclooxygenase Inhibitor.

TNF/IFNγ-IN-1 (TGA) is a dual inhibitor of TNF and IFN-γ. TNF/IFNγ-IN-1 has potential antioxidant and anti-inflammatory activities for neurodegenerative diseases such as Alzheimer.

Fenoprofen calcium is a propionic acid derivative that is used as a non-steroidal anti-inflammatory agent.

S-2474, an inhibitor of COX-2 and 5-lipoxygenase, has anti-inflammatory and neuroprotective activities and inhibits Abeta (25 - 35) and Abeta (1 - 40) induced cell death.

BN-82451 2HCl is a dual inhibitor of COX-1 and COX-2 and can be used to study Huntington's chorea and Parkinson's disease.

Coniferaldehyde can significantly inhibit the growth of viability of strains of Oenococcus oeni. Coniferaldehyde exerts anti-inflammatory properties by inducing heme oxygenase-1(HO-1).

COX-2-IN-34 is a selective, orally potent COX-2 inhibitor that shows anti-inflammatory activity without gastric ulcer toxicity during experiments in mice.

Nitroaspirin (NCX 4016) is a nitric oxide donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin induces significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins. Nitroaspirin has antithrombotic and antiplatelet properties and acts as a direct and irreversible inhibitor of COX-1.

SC-75416 is a selective COX-2 inhibitor for the study of pain.

Indomethacin farnesil (Infree) is a prodrug of indomethacin. It acts as a nonsteroidal anti-inflammatory drug (NSAID) and disease-modifying anti-rheumatic drug (DMARD).

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.

COX-2-IN-2, a selective inducible COX2 inhibitor, exhibits potent inhibition with an IC50 of 0.24 μM. Meanwhile, COX-2-IN-1 functions as an anti-inflammatory agent, demonstrating both anti-inflammatory and analgesic activities.

Floctafenine (R-4318) is an orally available nonsteroidal anti-inflammatory compound that is a COX-I and COX-2 inhibitor and interferes with the antiplatelet effects of aspirin.Floctafenine has analgesic activity and is used in the study of pain.

Amtolmetin guacil (ST-679) inhibits prostaglandin synthesis and cyclooxygenase. Amtolmetin guacil has similar NSAID properties like tolmetin with additional analgesic, antipyretic, and gastroprotective properties.

Lupeol acetate, a derivative of Lupeol, inhibits the progression of rheumatoid arthritis by downregulating TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.

Thioflosulide (L-745337) is a selective and potent COX2 inhibitor (IC50: 2.3 nM) with anti-inflammatory activity for the study of gastric ulcers.

6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.

Apyramide is an anti-inflammatory agent (NSAID) and behaves as a prodrug of indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2.

COX-2-IN-1 is a potent and selective COX-2 inhibitor (IC50: 3.9 μM).

Hamaline (9-(4-chlorobenzyl)-6-methoxy-1-methyl-4,9-dihydro-3H-pyrido[3,4-b]indole) is a substrate-selective cyclooxygenase-2 (COX-2) inhibitor.

4-Hydroxyantipyrine is formed during oxidative deamination of aminopyrine.

COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is used to prevent colorectal cancer. COX-2-IN-6 can be used to prevent colorectal cancer.

Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 μM. Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively).

Eltenac (B78820) is a non-steroidal anti-inflammatory, COX inhibitor with analgesic activity.Eltenac inhibits COX-1 and COX-2 and is used in the study of Acute Respiratory Distress Syndrome (ARDS).

Tenidap (CP-66248) is a selective COX-1 and SLC26A3 inhibitor with anti-inflammatory, analgesic, and anti-rheumatic activities.

RWJ 63556 is an orally active inhibitor of COX-2 selective/5-lipoxygenase, shows anti-inflammatory activities.

SC57666 is a highly selective COX2 inhibitor (IC50 at 26 nM) that shows no activity against COX1.

Meloxicam (Metacam) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of meloxicam is as a Cyclooxygenase Inhibitor. The chemical classification of meloxicam is Nonsteroidal Anti-inflammatory Compounds.

Zileuton (A 64077) is a synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma.

Acetaminophen (APAP) is a COX inhibitor that inhibits COX-1 and COX-2 (IC50=113.7/25.8 μM). Acetaminophen has antipyretic and analgesic activity as well as weak anti-inflammatory activity.