COX-2 Inhibitor

Dihydrokavain (7,8-Dihydrokawain) is a natural kavalactone compound. Dihydrokavain inhibits COX-1, COX-2, CYP2C9 (IC₅₀ = 130.95 μM), CYP2C19 (IC₅₀ = 10.05 μM) and CYP3A4 (IC₅₀ = 78.59 μM). Dihydrokavain reduces TNFα secretion. Dihydrokavain shows analgesic and anxiolytic effects.

Bromfenac sodium hydrate (Bromfenac monosodium salt sesquihydrate) is a potent and orally active inhibitor of COX, with IC₅₀s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac sodium hydrate can be used in ocular inflammation research.

Δ5-Avenasterol is an antioxidant that targets cyclooxygenase-2 (COX-2) and exists in tomato seed oil, oat grain oil, and wheat germ oil. Δ5-Avenasterol binds to the active site of COX-2, thereby blocking the conversion of arachidonic acid to inflammatory prostaglandins. Δ5-Avenasterol exerts antioxidant activity via the ethylene group at positions 24 and 28 of its side chain.

Saponarin is an orally active flavonoid compound. Saponarin can be isolated from Gypsophila trichotoma. Saponarin inhibits ERK/p38, NF-κB and MAPK phosphorylation and activates AMPK. Saponarin reduces IL-1β and COX-2. Saponarin has antioxidant, anti-inflammatory, hepatoprotective, hypoglycemic and hypotensive effects. Saponarin improves sleep disorders.

α-Spinasterol is an orally taken antagonist of transient receptor potential vanilloid 1 ( TRPV1), and it's also an inhibitor of COX-1 and COX-2, with IC₅₀ values of 16.17 μM and 7.76 μM, respectively. α-Spinasterol exhibits antibacterial, anti-inflammatory, antidepressant, and antioxidant effects, has the ability to cross the blood-brain barrier, and can improve diabetes in mice.

BMP-4 (15-24) acetate is a cell-penetrating heparin-binding peptide with the sequence RKKNPNCRRH. BMP-4 (15-24) acetate exhibits anti-inflammatory and anti-chondrogenic activities. BMP-4 (15-24) acetate can be used in the research of arthritis.

Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory agent on airway inflammation.

Asarylaldehyde (Asaronaldehyde), a COX-2 inhibitor, significantly inhibits cyclooxygenase II (COX-2) activity with an IC₅₀ value of 100 μg/mL.

Diclofenac acyl glucuronide (D-1-O-G) is an orally active glucuronide metabolite of Diclofenac (HY-15036). Diclofenac acyl glucuronide exhibits SOD inhibitory activity, COX-1 inhibitory activity (IC₅₀ = 0.620 μM), and COX-2 inhibitory activity (IC₅₀ = 2.91 μM). Diclofenac acyl glucuronide induces reactive oxygen species (ROS) production and acts as a substrate of OATP2B1. Diclofenac acyl glucuronide induces small intestinal ulcers. Diclofenac acyl glucuronide can be used in research related to intestinal diseases and small intestinal ulcers.

Diclofenac potassium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC₅₀s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac potassium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

Nepafenac (AHR 9434; AL 6515), a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC₅₀ of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC₅₀ = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE_₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries.

(S)-Flurbiprofen is an active enantiomer of Flurbiprofen, with IC₅₀ values of 0.48 μM and 0.47 μM for COX-1 and COX-2, respectively.

Pheophytin a is a multi-target inhibitor, anticancer agent, antioxidant and antiviral agent. Pheophytin a directly binds to and inhibits HCV-NS3/4A protease (IC₅₀=0.89 μM) to block viral replication. Pheophytin a also scavenges free radicals, reduces ferric ions, and exhibits cytotoxic activity against breast cancer cells. Pheophytin a effectively inhibits LPS-induced production of nitric oxide, prostaglandin E2, NOS2 and COX-2, as well as various pro-inflammatory cytokines, by downregulating the transcription levels of inflammatory mediators and blocking the ERK1/2 and STAT-1 pathways. In a low nerve growth factor environment, Pheophytin a also enhances ERK1/2 phosphorylation and synergistically promotes neurite outgrowth through MAPK pathway. Pheophytin a can be used to investigate the pathogenic mechanisms of diseases including chronic hepatitis C, sepsis, breast cancer and Alzheimer's disease.

Pelubiprofen is an orally active anti-inflammatory agent that inhibits COX enzyme activity (with IC₅₀ values of 10.66 and 2.88 μM for COX-1 and COX-2, respectively). Pelubiprofen has significant anti-inflammatory and analgesic effects.

Lupeol acetate is a derivative of Lupeol. Lupeol acetate is an anti-inflammatory, antibacterial, anti-trypanosomic and anticancer agent with oral activity. Lupeol acetate significantly improves the symptoms of rheumatoid arthritis by down-regulating the expression of inflammatory cytokines and osteoclast production. Lupeol acetate inhibits spermatogenesis in male rats and eventually led to infertility.

Tilmicosin (LY-177370) phosphate is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin phosphate mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin phosphate is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin phosphate has immunomodulatory and anti-inflammatory effects.

Aceclofenac is an orally active nonsteroidal anti-inflammatory agent (NSAID), with analgesic and anti-inflammatory properties. Aceclofenac is used for the research of osteoarthritis, ankylosing spondylitis, rheumatoid arthritis.

PTUPB is a potent and dual sEH and COX-2 enzymes inhibitor with IC₅₀ of 0.9 nM and 1.26 μM, respectively.

Methotrexate-d₃ is the deuterated-labeled Methotrexate (HY-14519). Methotrexate (Amethopterin; CL14377; WR19039) is an orally active antifolate (Antifolate). Methotrexate inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.

Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC₅₀s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor.