cox-1 selective

Vedaprofen (PM 150) inhibits COX-1 and reduces prostaglandin H2 synthesis with anti-inflammatory activities. Vedaprofen is an inhibitor of Escherichia coli sliding clamp with the IC50 of 222 μM and Ki of 131 μM.

COX-2-IN-2, a selective inducible COX2 inhibitor, exhibits potent inhibition with an IC50 of 0.24 μM. Meanwhile, COX-2-IN-1 functions as an anti-inflammatory agent, demonstrating both anti-inflammatory and analgesic activities.

COX-2-IN-1 is a potent and selective COX-2 inhibitor (IC50: 3.9 μM).

Tenidap (CP-66248) is a selective COX-1 and SLC26A3 inhibitor with anti-inflammatory, analgesic, and anti-rheumatic activities.

Aspirin is an orally active, selective, and irreversible inhibitor of COX-1 and COX-2 with IC₅₀ values of 5 and 210 μg/mL, respectively. It induces apoptosis, inhibits NF-κB activation and platelet prostaglandin synthesis, thereby preventing thrombosis. Additionally, it acts as a histone deacetylase inhibitor that upregulates p21, exhibiting anti-inflammatory, antipyretic, analgesic, and anti-platelet aggregation activities. Aspirin is commonly used to induce gastric ulcer models.

Diclofenac Diethylamine, a non-selective COX inhibitor, is utilized as a nonsteroidal anti-inflammatory drug (NSAID).

CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) is a potent and highly selective inhibitor of COX-2 and COX-1. It is also a potent inhibitor of PKB/Akt and MAPK signalling pathways and induces apoptosis in NSC-LC cells, with analgesic, anti-inflammatory and anti-cancer activities.

Ketorolac tromethamine salt (Ketorolac tris salt) non-selective inhibits the enzymes cyclooxygenase 1 (COX-1) and COX-2with anti-inflammatory, analgesic, and antipyretic activities.

HQL-79 is a selective and orally active human hematopoietic prostaglandin D synthase (H-PGDS) inhibitor. It inhibits the synthesis of PGD2 and acts as an anti-allergic agent (Kd: 0.8 μM and IC50: 6 μM). It also shows no obvious effect on COX-1, COX-2, m-P

Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor (IC50: 18 nM) that also inhibits COX-1 activity (IC50: 115 nM) and exhibits anti-inflammatory effects.

Pelubiprofen is an orally active, non-steroidal anti-inflammatory agent, a selective cyclooxygenase-2 (COX-2) inhibitor, which effectively reduces PGE(2) production by inhibiting COX activity. Pelubiprofen inhibits LPS-induced phosphorylation of IKK-β and transforming growth factor-β activated kinase-1 (TAK1).

Parecoxib sodium is a prodrug of Valdecoxib and a selective, orally active COX-2 inhibitor that suppresses prostaglandin (PG) synthesis and alleviates pain and inflammation. Parecoxib sodium also acts as a cannabinoid 1 (CB1) receptor agonist (EC50=2.4 µM).

HPGDS inhibitor 1 is a novel and selective inhibitor for Hematopoietic Prostaglandin D Synthase (HPGDS) with an IC50 Value of 0.7 nM.

Ketorolac (RS37619) hydrochloride is a nonsteroidal anti-inflammatory drug and a non-selective COX inhibitor, exhibiting IC50 values of 20 nM for COX-1 and 120 nM for COX-2. This compound is utilized in a 0.5% ophthalmic solution format for the investigation of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and post-operative ocular inflammation pain. Additionally, Ketorolac hydrochloride serves as a DDX3 inhibitor, making it pertinent for research in cancer therapies.

AGU654 (Compound 44) is a selective mPGES-1 inhibitor with an IC50 value of 2.9 nM against mPGES-1. By inhibiting mPGES-1, AGU654 interrupts the pathway where COX-1/2 converts arachidonic acid to prostaglandin E2 (PGE2), effectively reducing inflammatory responses, pain, and fever symptoms. In models using activated human monocyte-derived macrophages and whole blood, AGU654 selectively inhibits PGE2 production induced by bacterial endotoxins, while preserving the production of other prostaglandins. In guinea pig models, AGU654 significantly alleviates fever, inflammation, and inflammatory pain, demonstrating excellent anti-inflammatory, analgesic, and antipyretic effects. AGU654 holds promise as a new approach for researching inflammatory diseases and pain.

WYZ90 (compound 6a) is a potent and selective COX-2 inhibitor, with IC50 values of 75 nM for COX-2, 5734 nM for COX-1, and 19940 nM for DPPH. It also exhibits antioxidant and analgesic activities.

COX-2-IN-41 (compound 5e) is a selective COX-2 inhibitor with an IC50 value of 1.74 μM. It demonstrates selectivity over COX-1, with a selectivity ratio of IC50(COX-1)/IC50(COX-2) = 16.32.

COX-2-IN-56 (example 6) is a selective COX-2 inhibitor that shows no significant inhibitory effect on COX-1. It can be utilized in research on COX-2-dependent conditions such as inflammation.

Desmethyl etoricoxib (example 21) is a selective COX-2 inhibitor with an IC50 greater than 1 μM in whole blood. It exhibits inhibitory activity against COX-1, with an IC50 of 16 μM in U937 cells, and demonstrates anti-inflammatory properties.

COX-1ligand 1 (Compound 44) is a selective COX-1 ligand with a binding affinity (Kd or Ki value) of 22 nM for rhesus monkey COX-1 and 43 nM for human COX-1. It inhibits the binding of [3H]PS13 to human COX-1. When labeled with either 11C or 18F, COX-1ligand 1 can be utilized for COX-1 imaging and psychiatric disorder research.

COX-1-IN-5 (example 13, compound PS13) is a potent and selective COX-1 inhibitor with an IC50 of 1 nM, significantly more selective for COX-1 over COX-2 (COX-2 IC50 > 0.1 μM) by over 1000-fold. It demonstrates substantial anti-inflammatory, antipyretic, analgesic, antithrombotic, and anticancer activities. COX-1-IN-5 is applicable in the study of COX-mediated diseases such as inflammation and pain. When radiolabeled with 11C, it serves as a selective PET tracer for systemic imaging of COX-1 distribution and target binding in vivo.

ML351 is a potent and selective inhibitor of human 15-lipoxygenase-1 (15 LOX)(IC50: 200 nM).

Indomethacin heptyl ester is a non-selective inhibitor of both COX-1 and COX-2

FR 122047 (1-[(4,5-Bis(4-methoxyphenyl-2-thiazoyl)carbonyl]-4-methylpiperazine, Hydrochloride) is a potent and selective inhibitor of COX-1 with IC50 of 28 nM and 65 µM for human recombinant COX-1 and COX-2, respectively.