MS-PPOH

MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor[1]. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively[2].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

Research Areas >> Metabolic Disease

Research Areas >> Neurological Disease

MS-PPOH blocks cellular EET synthesis. MS-PPOH inhibits tonic (basal) cell invasion and migration and reduces the 11,12-EET (1.0 μM)-induced cell motility[1]. Cell Viability Assay[1] Cell Line: PC-3 cells Concentration: 2.0 and 10.0 μM Incubation Time: 24 hours Result: Inhibited tonic (basal) cell invasion and migration.

MS-PPOH (20 mg/kg/day, i.v.) for 6 days significantly reduced renal levels of epoxyeicosatrienoic acids (EETs) in Dahl salt-resistant rats on 2% NaCl drinking solution[3]. Animal Model: Six-week-old male stroke-prone spontaneously hypertensive rats (SHRSP)[3] Dosage: 20 mg/kg/day Administration: Intravenously Result: Treatment had negligible effects on systolic blood pressure (SBP) in saline-drinking SHRSP after 1 week, 160 vs. 167 mmHg, or 2 weeks of treatment, 171 vs. 175 mmHg, for vehicle vs. MS-PPOH, respectively.

[1]. Kasem Nithipatikom, et al. Inhibition of carcinoma cell motility by epoxyeicosatrienoic acid (EET) antagonists. Cancer Sci. 2010 Dec;101(12):2629-36.

[2]. Jun Yang, et al. Cytochrome P450 2C24: Expression, Tissue Distribution, High-Throughput Assay, and Pharmacological Inhibition. Acta Pharm Sin B. 2012 Apr;2(2):137-145.

[3]. Jing Li, et al. Pharmacological manipulation of arachidonic acid-epoxygenase results in divergent effects on renal damage. Front Pharmacol. 2014 Aug 15;5:187.