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.

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

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

Chlorotrianisene (tri-p-anisylchloroethylene) is an orally bioavailable, highly lipophilic, synthetic triphenylethylene (TPE) derivative and selective estrogen receptor modulator (SERM), with predominantly estrogenic but also antiestrogenic activities.

Lumiracoxib (Prexige) is a novel, selective COX-2 inhibitor with IC50 and Ki of 0.14 μM and 0.06 μM, exhibits 515-fold selectivity over COX-1. Phase 4.

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

TFAP (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) is a selective cyclooxygenase-1 (COX-1) inhibitor

Hamaline (9-(4-chlorobenzyl)-6-methoxy-1-methyl-4,9-dihydro-3H-pyrido[3,4-b]indole) is a substrate-selective cyclooxygenase-2 (COX-2) inhibitor.

SC-236 (Sc 236) is an orally active and selective inhibitor of COX-2 (IC50 of 0.005 μM and 17.8 μM for COX-2 and COX-1, respectively).

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).

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.

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.

5-hydroxy Diclofenac is a metabolite of the NSAID diclofenac formed by the cytochrome P450 (CYP) isoform CYP3A4. Diclofenac is a non-selective COX inhibitor. It inhibits human COX-1 and -2 with IC50 values of 0.9-2.7 and 1.5-20 μM, respectively. Diclofenac inhibits ovine COX-1 and -2 with IC50 values of 60 and 220 nM, respectively.

Mofezolac (formerly known as Disopain or N-22) is a highly selective COX-1 (cyclooxygenase-1) inhibitor with COXs selectivity index > 6000

Ibuprofen ((±)-Ibuprofen) sodium is an orally active, selective inhibitor of COX-1 (IC50 = 13 μM) that inhibits cell proliferation and angiogenesis, and induces cell apoptosis. It is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor, used in research on pain, swelling, inflammation, infection, immunology, and cancers [1] [2] [5] [8].