List of Cyclooxygenase (COX) Inhibitors
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| Cyclooxygenase (COX) Inhibitors | |||
|---|---|---|---|
| COX-1 Inhibitor, FR122047 (4,5-Bis(4-methoxyphenyl-2-[(1-methylpiperazin-4-yl)carbonyl]thiazole, HCl) |
236005 | A cell-permeable, potent, and selective inhibitor of COX-1 (IC50 = 28 nM) with much lower selectivity for COX-2 (IC50 = 65 µM).. | 5 mg |
| COX-1 Inhibitor II (4-Amino-(N-(4-cholorophenyl)-N-methyl)benzenesulfonamide) |
236006 | A cell-permeable, catalytic site targeting, COX-1-selective inhibitor(IC50 = 3.2 µM and >100 µM for COX-1 and COX-2, respectively). | 25 mg |
| COX-2 Inhibitor I (Methyl [5-methylsulfonyl-1-(4-chlorobenzyl)-1H-2-indolyl]carboxylate) |
236011 | A cell-permeable, selective inhibitor of COX-2 (IC50 = 650 nM) over COX-1 (IC50 > 10 µM). | 5 mg |
| COX-2 Inhibitor II (4-[(5-Difluoromethyl-3-phenyl)-4-isoxazolyl]benzenesulfonamide) |
236012 | A cell-permeable, potent, and highly selective inhibitor of COX-2 both in vitro; (IC50 = 4 nM for hCOX-2 vs. 114 µM for hCOX-1) and in vivo. | 5 mg |
| COX-2 Inhibitor III (N-(5-Acetyl-2-piperidinophenyl)-N′-(2,5-dichlorophenyl)thiourea) |
236013 | An active-site-targeting COX-2 inhibitor that exhibits better selectivity than Nimesulide and Celecoxib. (% inhibition of COX-1 and COX-2 at 10.0 µM inhibitor concentration = 5.1 and 26.36%, respectively). | 25 mg |
| COX-2 Inhibitor IV (5-(4-Methoxyphenyl)-3,7-dimethyl-4,5-dihydroisoxazolo[4,5-d]pyridazin-4-one) |
236014 | An active-site-targeting COX-2 inhibitor with potency and selectivity over COX-1 (33.85% inhibition of COX-2 at 10.0 µM). | 25 mg |
| COX-2 Inhibitor V, FK3311 (4′-Acetyl-2′-(2,4-Difluorophenoxy) methanesulfonanilide) |
236015 | A cell-permeable, COX-2-selective inhibitor that with 500-fold greater potency in inhibiting the LPS-induced TxB2 production (IC50 = 316 nM) compared to the non-induced/constitutive TxB2 (IC50 = 160 µM). | 5 mg |
| Diclofenac, 4’-Hydroxy- (2-[((2′,6′-Dichloro-4′-hydroxy) phenyl)amino]benzeneacetic Acid) |
287845 | A cell-permeable metabolite of Diclofenac that act as a potent inhibitor of COX 2 (IC50 = 16.9 nM). | 100 µg |
| Diclofenac Sodium (2-[(2,6-Dichlorophenyl)amino]benzeneacetic Acid, Sodium) |
287840 | A cell-permeable, non-selective COX inhibitor (IC50 = 60 nM and 200 nM for ovine COX-1 and COX-2 respectively). | 1 g |
| DuP-697 (5-Bromo-2-(4-fluorophenyl)-3-(4-(methylsulfonyl)phenyl)thiophene) |
317500 | A cell permeable, potent, irreversible, and time-dependent COX-2 inhibitor with over 50-fold greater inhibitory potency against human and murine recombinant COX-2 (IC50 = 80 nM and 40 nM at 5 and 10 min respectively) than COX-1 (IC50 = 9 µM). | 5 mg |
| Ebselen (2-Phenyl-1,2-benzisoselenazol-3(2H)-one) |
324483 | A cell-permeable, seleno-organic compound that acts as a non-selective inhibitor of both COX-1 and COX-2. | 5 mg |
| Flurbiprofen (±)-2-Fluoro-a-methyl[1,1′-biphenyl]-4-acetic Acid) |
344079 | A mixture of S(+) and R(–) enantiomers. A cell-permeable, potent and non-selective inhibitor of cyclooxygenases. | 100 mg |
| (±)-Ibuprofen | 401003 | A reversible and competitive inhibitor of COX-1 (IC50 = 4.85 µM). Inhibits COX-2 at higher concentrations (IC50 = 223 µM). | 1 g |
| Indomethacin 1-(p-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic Acid |
405268 | A cell permeable, non-selective inhibitor of COX (IC50 = 740 nM for COX-1; IC50 = 970 nM for COX-2). | 10 g |
| Indomethacin Ester, 4-Methoxyphenyl- (1-(p-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic Acid, 4-Methoxyphenyl Ester |
405271 | A cell-permeable 4-methoxyphenyl ester derivative of Indomethacin that acts as a potent and selective inhibitor of COX-2 (IC50 = 40 nM) compared to COX-1 (IC50 > 66 µM). | 5 mg |
| Kaempferol (3,4′,5,7-Tetrahydroxyflavone) |
420345 | A cell-permeable inhibitor of COX-1 activity (IC50 = 180 µM). Also blocks the transcriptional activation of COX-2 (IC50 <5 µM). | 25 mg |
| MEG Hydrochloride (Mercaptoethylguanidine, HCl) |
444600 | A cell-permeable inhibitor of inducible nitric oxide synthase (iNOS) and a peroxynitrite scavenger that also causes a dose-dependent inhibition of COX-1 (IC50 = 20 µM) and COX-2 activity. | 10 mg |
| Meloxicam (4-Hydroxy-2-methyl-N-(5-methyl-2-thiazoyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide) |
444800 | A cell-permeable, selective inhibitor of COX-2 (IC50 = 4.7 µM) compared to COX-1 (IC50 = 36.6 µM). | 100 mg |
| NS-398 (N-(2-Cyclohexyloxy-4-nitrophenyl) methanesulfonamide |
349254 | A cell-permeable, selective inhibitor of COX-2 (IC50 = 3.8 µM). Does not affect COX-1 activity even at 100 µM. | 5 mg |
| Parthenolide, Tanacetum parthenium | 512732 | A cell-permeable inhibitor of COX-2 and proinflammatory cytokines (TNF-α and IL-1) expression in LPS-stimulated macrophages. | 50 mg |
| Pterostilbene, Pterocarpus marsupium (trans-3,5-Dimethoxy-4′-hydroxystilbene) |
523310 | A cell-permeable methoxylated analog of Resveratrol (Cat. No. 554325) that moderately inhibits COX-1 and -2 activities (IC50 = 19.8 µM and 83.9 µM) respectively. | 10 mg |
| Radicicol, Diheterospora chlamydosporia | 553400 | An antifungal macrocyclic lactone antibiotic that inhibits the expression of COX-2 (IC50 = 27 nM) without affecting COX-1 expression in LPS-stimulated macrophages. | 500 µg |
| Resveratrol (trans-3,4′,5-Trihydroxystilbene) |
554325 | A specific inhibitor of COX-1 (ED50 = 15 µM). Also inhibits the hydroxyperoxidase activity of COX-1 (ED50 = 3.7 µM). | 25 mg |
| SC-560 (5-(4-Chlorophenyl)-1-(4-methoxyphenyl)-3-trifluoromethylpyrazole) |
565610 | A cell-permeable, highly potent, and selective inhibitor of COX-1 (IC50 = 9 nM) over COX-2 (IC50 = 6.3 µM). | 5 mg |
| Sodium Salicylate | 567630 | A cell-permeable weak inhibitor of COX-2 (IC50 = 100 µM). | |
| Sulindac Sulfide ((Z)-5-Fluoro-2-methyl-1-[p-(methylthio)benzylidene]indene-3-acetic Acid) |
574102 | A cell-permeable, selective, potent inhibitor of COX-1 (ID50 = 500 nM) over COX-2 (IC50 = 14 µM). | 5 mg |
| Sulindac Sulfone ((Z)-5-Fluoro-2-methyl-1[p-(methylsulfonyl) benzylidene]indene-3-acetic Acid) |
574105 | A cell-permeable sulfone metabolite of Sulindac (Cat. No. 574100) that has anticancer properties but lacks COX inhibitory activity. | 5 mg |
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Cyclooxygenase Inhibitor Set Cat. No. 239783 1 set |
Also Available...
COX-2 ELISA Kit, Cat. No.
A 96-well complete kit for the quantitative determination of human COX-2 in cell lysates. The 96-well plate is coated with a rabbit anti-human COX-2 polyclonal antibody as the capture antibody. Standards and samples are added to the wells at which time COX-2 is bound to the coated antibody. COX-2 is then detected with a monoclonal anti-COX-2 antibody and a goat anti-mouse IgG HRP Conjugate. The addition of TMB Substrate results in a blue-colored product in the presence of the HRP Conjugate. Sensitivity is increased by the addition of ELISA Stop Solution (H2SO4), yielding a yellow color. The absorbance of each well is measured at 450 nm (preferably with reference wavelength set of 540-600 nm).
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A standard curve was generated according to the COX-2 Standard preparation and the Detailed Protocol above. The results represent a typical standard curve. Assay range: 2.5-200 ng/ml. Lower limit of detection: ~2 ng/ml. Assay Range: 2.5-200 ng/ml |
