Drug intelligence / Profile preview

PTUPB

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

PTUPB is a potent, selective dual inhibitor of soluble epoxide hydrolase (sEH) and cyclooxygenase-2 (COX-2). It exhibits IC50 values of approximately 0.9 nM for sEH and 1.26 μM for COX-2, with high selectivity over COX-1[1][2][3][4]. Mechanistically, PTUPB blocks both the sEH and COX-2 pathways, which are implicated in inflammation, fibrosis, angiogenesis, tumor growth, and vascular remodeling[5][6]. Preclinical studies have demonstrated anti-tumor effects (notably in lung cancer models), anti-inflammatory activity (including suppression of NLRP3 inflammasome activation), attenuation of liver fibrosis and portal hypertension in cirrhosis models, as well as reduction of epithelial-mesenchymal transition in pulmonary fibrosis models[5][6]. The compound has also shown efficacy in reducing renal inflammation and oxidative stress. PTUPB is primarily used as a research tool; it is not approved for clinical use.

Other names
4-(5-phenyl-3-{3-[3-(4-trifluoromethylphenyl)-ureido]-propyl}-pyrazol-1-yl)-benzenesulfonamide
02

Targets

EPHX2 (Soluble epoxide hydrolase)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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