COX Control

Zaloglanstat (ISC-27864; GRC-27864) is a selective, orally active microsomal mPGES-1 inhibitor. Zaloglanstat has an IC₅₀ of 5 nM for human mPGES-1 without significant inhibitory effect on COX-1/2 (IC₅₀ >10 μM). Zaloglanstat blocks the conversion of arachidonic acid metabolite prostaglandin PGH₂ to prostaglandin PGE₂, thereby inhibiting inflammation-related PGE₂ overproduction and reducing inflammatory responses and pain. Zaloglanstat inhibits IL-1β-induced PGE₂ release in A549 cells and human synovial fibroblasts in vitro. Zaloglanstat inhibits PGE2 release in pig and dog whole blood with IC₅₀s of 161 nM and 154 nM, respectively. Zaloglanstat can be used in the study of asthma, osteoarthritis, and neurodegenerative diseases.

p-Ethylhydratropic acid (compound 5b) is the impurity of Ibuprofen (HY-78131). Ibuprofen is a potent, orally active, selective COX-1 inhibitor.

6-Hydroxy etodolac (compound 2) is a metabolite of Etodolac (HY-76251). Etodolac is a non-steroidal anti-inflammatory compound and is a COX inhibitor.

5'-Hydroxy meloxicam is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) Meloxicam (HY-B0261).

Hydroxycelecoxib glucuronide is the glucuronide metabolite of Celecoxib (HY-14398) and shows no activity in inhibiting COX-2 activity.

T26A is a highly selective prostaglandin transporter (PGT) inhibitor.T26A does not interact with the PGT homolog OATPc, blocks PGT-mediated PGE₂ influx, and blocks PGE₂ metabolism.T26A retains PGE₂ in the extracellular compartment and reduces intracellular PGE₂ metabolites.T26A elevates circulating endogenous PGE₂ levels, reduces circulating endogenous PGE₂ metabolite levels, and slows metabolism of exogenously injected PGE₂ in Rattus norvegicus via intravenous injection.T26A does not affect PGE₂ synthesis.T26A can be used for the research of PGT function in adult animals.

Aceclofenac ethyl ester is an impurity of Aceclofenac (HY-B0634).

(±)-Ketoprofen glucuronide is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) Ketoprofen (HY-B0227).