Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively)[1]. Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM[2].
COX-2/5-LOX-IN-1 (compound 3a) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-1 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-1 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-1 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 12.13, 0.4 and 4.96 μM, respectively[1].
COX-2-IN-14 (compound 2a) is a potent and selective COX-2 (cyclooxygenase-2) inhibitor. COX-2-IN-14 shows effective binding at the active site of COX-2 co-crystal. COX-2-IN-14 exhibits a high level of in vivo anti-inflammatory activity, reducing ear edema and myeloperoxidase (MPO) activity in mice[1].
Ketorolac D4 (RS37619 D4) is the deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2[1][2].
NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.
Ketorolac D5 is a deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2[1].
Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities.
Ketoprofen (RP-19583) lysinate is a non-steroidal anti-inflammatory agent. Ketoprofen lysinate can inhibit the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity[1][2][3].
Ermanin is a flavonoid isolated from Tanacetum microphyllum. Ermanin potently inhibits iNOS, COX-2 activities, and inhibits platelet aggregation. Ermanin has anti-inflammatory, anti-tuberculous and anti-viral/bacterial properties[1][2].
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta[1].Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models[2], has selective inhibitory activity towards cyclooxygenase-2 (COX-2)[1].Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways[3].
Ethyl Caffeate is a natural phenolic compound isolated from Bidens pilosa. Ethyl caffeate suppresses NF-κB activation and its downstream inflammatory mediators, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and prostaglandin E2 (PGE2) in vitro or in mouse skin[1].
Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects[1].
Veratric acid-d6 is deuterium labeled Veratric acid. Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant[1] and anti-inflammatory activities[3]. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling[2]. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation[3].
Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 μM, respectively. Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.
Ibuprofen D3 is a deuterium labeled Ibuprofen. Ibuprofen is a COX-1 and COX-2 inhibitor with IC50s of 13 μM and 370 μM[1].
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 drug on airway inflammation[1].
COX-2-IN-22 (Compound 4h) is a COX-2 inhibitor with an IC50 of 8.6 µM. COX-2-IN-22 also inhibits AChE, BChE, β-Secretase, LOX-5 and DPPH with IC50 values of 2.8, 6.3, 15.3, 13.9 and 6.8 µM, respectively. COX-2-IN-22 can cross BBB[1].
Ibuprofen-13C,d3 is the 13C- and deuterium labeled. Ibuprofen is an anti-inflammatory agent targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
Anti-inflammatory agent 56 (Compound 9) is a selective COX-2 inhibitor (IC50: 0.54 μM). Anti-inflammatory agent 56 has anti-oxidant and anti-inflammatory effects. Anti-inflammatory agent 56 inhibits oxidative stress induced cell death. Anti-inflammatory agent 56 inhibits oxidative stress and neuroinflammation by inhibiting Keap1, COX-2 and iNOS. Anti-inflammatory agent 56 has low acute toxicity in mice (LD50: 1000 mg/kg)[1].
Ibuprofen ((±)-Ibuprofen) L-lysine is a potent orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen L-lysine inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen L-lysine is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen L-lysine can be used in the research of pain, swelling, inflammation, infection, immunology, cancers[1][2][3][4][5][6][7][8].
Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis[1]. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL[2]. Anti-hyperglycemic and anti-inflammatory activities[1].
Shizukaol B is a lindenane-type dimeric sesquiterpene, used to be isolated from the whole plant of Chloranthus henryi. Shizukaol B has anti-inflammatory effect against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells. Shizukaol B inhibits iNOS and COX-2, and suppresses NO production, TNF-α, and IL-1β expression[1].
Nimesulide D5 is a deuterium labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties[1][2].
AL-8417 is an enzyme inhibitor. It acting as an antioxidant, anti-inflammatory, and cytostatic agent. It also has the ability to suppress vitrectomy-induced posterior lens fiber changes.
Moracin C, a natural product, is an anti-inflammatory agent. Moracin C inhibits LPS-activated reactive oxygen species (ROS) and nitric oxide (NO) release from cells[1].
Phenylbutazone-d10 (diphenyl) is the deuterium labeled Phenylbutazone. Phenylbutazone is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Phenylbutazone, a hepatotoxin, is a nonsteroidal anti-inflammatory drug (NSAID). Phenylbutazone induces muscle blind-like protein 1 (MBNL1) expression and has the potential for ankylosing spondylitis research[1][2].
Pectolinarigenin, isolated from Cirsium chanroenicum, is a dual inhibitor of COX-2/5-LOX. Anti-inflammatory activity[1]. Pectolinarigenin has potent inhibitory activities on melanogenesis[2].
Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes 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[1][2][3][4].
Taraxerol acetate is a COX-1 and COX-2 inhibitor with IC50 values of 116.3 μM and 94.7 μM, respectively. Taraxerol acetate the has the anticancer potential and induces cell apoptosis[1].
Indomethacin heptyl ester is a selective COX-2 inhibitor with IC50 of 0.04 μM, exhibits anti-inflammatory activity[1].