COX-2 Inhibitor

Crocetin (Standard) (TransCrocetin (Standard) ) is an aglycone of crocin. Crocetin (Standard) is orally active and brain-penetrant. Crocetin (Standard) shows strong NMDA receptor affinity and channel opening activity. Crocetin (Standard) can downregulate the proinflammatory cytokines and COX-2 exoression. Crocetin (Standard) can inhibit apoptosis and activation of MAPK. Crocetin (Standard) can delay delays brain and body aging. Crocetin (Standard) can be used for the researches of cancer, neurological disease and inflammation, such as cervical cancer and ischemia.

Ocarocoxib is a potent cyclooxygenase-2 (COX-2) inhibitor (IC₅₀: 1.4 μM). Ocarocoxib inhibits COX to block the production of prostaglandins, thus exerting an anti-inflammatory effect. Ocarocoxib has potential in the study of inflammation and related diseases.

Tebufelone (NE-11740), a nonsteroidal anti-inflammatory drug (NSAID), is a selective dual COX-2/5-lipoxygenase inhibitor. Tebufelone displays potent anti-inflammatory, analgesic and anti-pyretic properties.

Amfenac Sodium Hydrate is a COX-2 inhibitor.

Indomethacin-d₄ (Indometacin-d₄) is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable 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. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.

Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs.

(S)-(+)-Ibuprofen-d₃ is a deuterium labeled (S)-(+)-Ibuprofen. (S)-(+)-Ibuprofen is the S(+)-enantiomer of Ibuprofen that inhibits COX-1 and COX-2 activity with IC₅₀s of 2.1 μM and 1.6 μM. (S)-(+)-Ibuprofen has analgesic, antiinflammatory and antipyretic effects.

1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is an AP-1 inhibitor which can be found in Cordyceps bassiana. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid downregulates the expression of COX-2. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid can be used for the study of atopic dermatitis.

GW406381, a highly selective cyclooxygenase-2 (COX-2) inhibitor, attenuates spontaneous ectopic discharge in sural nerves of rats following chronic constriction injury.

Anemarsaponin B is a steroidal saponin. Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .

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.

Hamaudol is a chromone isolated from Saposhnikovia divaricata. Hamaudol shows significant inhibitory activity on cyclooxygenase (COX)-1 and COX-2 activities with IC₅₀ values of 0.30, 0.57 mM, respectively, and has potent analgesia and anti-inflammary effects.

Cimicoxib (UR-8880) is an orally active, blood-brain barrier-permeable COX-2 inhibitor that also exerts targeted inhibition on CYP2D15. It has an IC₅₀ of 66 nM against hCOX-2, an IC₅₀ of 1.6 μM against canine CYP2D15, and an IC₅₀ of 0.056 μM against feline CYP2D15. By inhibiting the COX-2 pathway to reduce the production of thromboxane B2 and prostaglandin E2, Cimicoxib exerts antipyretic, anti-inflammatory and analgesic effects. Cimicoxib is metabolized by CYP2D15 to form demethyl-cimicoxib, undergoes glucuronidation via UDP-glucuronosyltransferases, and exhibits biphasic elimination kinetics in beagle dogs. Cimicoxib is widely used in studies of inflammatory diseases, osteoarthritis, and perioperative pain associated with orthopedic or soft tissue surgeries.

3,9-Dihydroeucomin (compound 12) is a natural homoisoflavonoid compound with less COX-2 inhibitory activitys.

Guluronic acid (G2013) is an orally active oxidative stress regulator and anti-inflammatory agent that exerts pharmacological effects by down-regulating various pro-inflammatory and oxidative stress-related genes (such as TLR4, NF-κB, iNOS, etc.) and inhibiting the activities of COX-2, MMPs and VEGF. Low-dose Guluronic acid up-regulates the expression of immunoregulatory genes SHIP1 and SOCS1, thereby effectively inhibiting cancer-related inflammation, tumor angiogenesis, cell adhesion and metastasis, while reducing the accumulation of immunosuppressive cells. Guluronic acid significantly prolongs the survival time of tumor-bearing hosts within a concentration range without direct cytotoxicity, demonstrating favorable safety. Guluronic acid has involved in the research of multiple sclerosis, ankylosing spondylitis, breast cancer and other inflammatory diseases.

Cucurbitacin R is an orally active anti-inflammatory agent. Cucurbitacin R is isolated from the roots of Cayaponia tayuya. Cucurbitacin R inhibits Cyclooxygenase-2. Cucurbitacin R inhibits Interleukin-6-induced STAT3 activation and cytokine production, blocks NF-κB activation, and selectively prevents NFAT nuclear translocation without affecting Calcineurin activity. Cucurbitacin R inhibits TNF-α production and Nitric-oxide synthase-2 expression. Cucurbitacin R reduces joint damage, soft tissue swelling, paw edema, ear edema, inflammatory cell infiltration, and epithelial thickness. Cucurbitacin R can be used for research on arthritis and delayed-type hypersensitivity.

Methotrexate-d₃ diammonium 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.

Ro 106-9920 is an orally active NF-κB inhibitor. Ro 106-9920 prevents ubiquitination of IκBα, blocks nuclear translocation of NF-κB, and inhibits NF-κB activation. Ro 106-9920 suppresses TNF-α-induced tissue factor expression and procoagulant activity, enhances TNF-α-mediated cytotoxicity against cancer cells, and eliminates the formation of neutrophil extracellular traps. Ro 106-9920 inhibits NLRP3 inflammasome activation, reduces inflammatory cytokine secretion, decreases myeloperoxidase activity, attenuates renal cell apoptosis, and improves renal function. Ro 106-9920 blocks ANG II (Angiotensin II human) (HY-13948)-induced nuclear localization of p65, internalization of AT_1A receptor, colocalization of β-arrestin-2, and expression of COX-2, and alters the formation of β-arrestin endosomes. Ro 106-9920 can be used in research related to non-small cell lung cancer, acute kidney injury, diabetes mellitus, and osteoporosis.

Gaultherin is an orally active non-steroidal anti-inflammatory agent. Gaultherin selectively inhibits NF-κB, MAPK, COX-2 (IC₅₀ = 0.35 mg/mL), LOX (IC₅₀ = 0.56 mg/mL) and HYAL (IC₅₀ = 28.58 μg/mL) to exert anti-inflammatory, antipyretic and analgesic effects. Gaultherin exhibits modest direct antioxidant capacity, greater in cell-based models. Gaultherin does not affect COX-1 so that avoids the common gastrointestinal side effects of Aspirin (HY-14654).

SC57666 is a selective COX2 inhibitor with an IC₅₀ of 26 nM.