COX-1 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S5192 S-(+)-Ketoprofen

S-(+)-Ketoprofen (Compound 1, Actron, (S)-Ketoprofen, Dexketoprofen) is a potent inhibitor of cyclooxygenase (COX) with IC50 of 1.9 nM and 27 nM for COX-1 and COX-2, respectively.

Selective COX-1, IC50: 1.9 nM
S6686 SC-560

SC-560 is a highly selective COX-1 inhibitor with IC50 of 9 nM, compared with the IC50 of 6.3 μM for COX-2, nearly 1,000-fold higher than with COX-1.

Selective COX-1, IC50: 9 nM
S1723 Indomethacin (NSC-77541)

Indomethacin (NSC-77541, Indometacin) is a nonselective COX1 and COX2 inhibitor with IC50 of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling.

Selective COX1, IC50: 0.28 μM
S6780 TFAP

TFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) is a selective and cell-permeable cyclooxygenase-1 (COX-1) inhibitor with IC50 of 0.8 μM.

Selective COX-1, IC50: 0.8 μM
S1638 Ibuprofen (NSC 256857)

Ibuprofen (NSC 256857, Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.

Selective COX-1, IC50: 13 μM
S3200 Triflusal

Triflusal (UR1501) irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1.

Selective
S2351 Salicin

Salicin (Salicoside, Salicine) is a phenol β-glycosid produced from willow bark that shows anti-inflammatory effects. It is a natural, non-selective COX-1 and COX-2 inhibitor.

Pan
S2047 Lornoxicam

Lornoxicam (Chlortenoxicam) is a non-steroidal COX-1/COX-2 inhibitor, used as an anti-inflammatory drug to treat pain, osteoarthritis, and rheumatoid arthritis.

Pan COX-1, IC50: 5 nM
S5698 Ketorolac tromethamine salt

Ketorolac tromethamine is a synthetic pyrrolizine carboxylic acid derivative with anti-inflammatory, analgesic and antipyretic properties. It is a non-selective COX inhibitor with IC50s of 20 nM for both COX-1 and COX-2.

Pan COX1, IC50: 20 nM
S4295 Meclofenamate Sodium

Meclofenamate Sodium is a dual COX-1/COX-2 inhibitor with IC50 of 40 nM and 50 nM, respectively, used in the treatment of joint, muscular pain, arthritis and dysmenorrhea. Meclofenamate Sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor.

Pan COX-1, IC50: 40 nM
S1903 Diclofenac Sodium

Diclofenac Sodium (GP 45840) is a non-selective COX inhibitor with IC50 of 0.5 μg/ml and 0.5 μg/ml for COX-1 and -2 in intact cells, respectively, used as a nonsteroidal anti-inflammatory drug (NSAID) to relieve pain and reduce swelling in flammation.

Pan COX-1, IC50: 60 nM
S5010 Indometacin Sodium

Indometacin Sodium (Indomethacin Sodium) is the sodium salt of indomethacin, which is a non-selective, reversible, and competitive inhibitor of cyclooxygenases 1 and 2 with anti-inflammatory, analgesic-antipyretic and tocolytic effects.

Pan COX1, IC50: 0.11 μM
S4149 Amfenac Sodium Monohydrate

Amfenac Sodium monohydrate is a non-steroidal analgesic anti-inflammatory drug with acetic acid moiety. The IC50 values for COX1 and COX2 is 250 nM and 150 nM, respectively.

Pan COX-1, IC50: 250 nM
S1396 Resveratrol (SRT501)

Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.

Pan COX1, IC50: 1.1 μM
S1646 Ketorolac

Ketorolac is a non-selective COX inhibitor of COX-1 and COX-2 with IC50 of 1.23 μM and 3.50 μM, respectively.

Pan COX-1 (human), IC50: 1.23 μM
S2903 Lumiracoxib

Lumiracoxib (COX-189) is a novel, selective COX-2 inhibitor with Ki of 0.06 μM. It also inhibits COX1 with Ki of 3 μM.

Pan COX-1, Ki: 3 μM
S1626 Naproxen Sodium

Naproxen Sodium (RS-3650) is a COX inhibitor for COX-1 and COX-2 with IC50 of 8.7 μM and 5.2 μM, respectively.

Pan COX-1, IC50: 8.7 μM
S4248 Bromfenac Sodium

Bromfenac Sodium (AHR 10282R) is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity and may block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2.

Pan
S1645 Ketoprofen

Ketoprofen (RP-19583) is a dual COX1/2 inhibitor, used as a nonsteroidal anti-inflammatory drug to treat arthritis-related inflammatory pains.

Pan
s7889 Xanthohumol

Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1.

Pan
S4230 Oxaprozin

Oxaprozin (WY-21743) is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID) used to relieve the inflammation, swelling, stiffness, and joint pain associated with osteoarthritis and rheumatoid arthritis.

Pan
S3008 Zaltoprofen

Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis.

Pan
S1761 Suprofen

Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.

Pan
S3017 Aspirin (NSC 27223)

Aspirin (NSC 27223, Acetylsalicylic acid, ASA) is a salicylate, and irreversible COX1 and COX2 inhibitor, used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin induces autophagy and stimulates mitophagy.

Pan
S1255 Nepafenac

Nepafenac (AHR 9434, AL 6515) is a prodrug of amfenac that acts as an inhibitor of COX-1 and COX-2 activity, used in the treatment of pain and inflammation associated with cataract surgery.

Pan
S4078 Mefenamic Acid

Mefenamic Acid (CI 473, CN-35355) is a competitive inhibitor of COX-1 and COX-2.

Pan