Flumethasone

Flumethasone (Flumetasone) is an orally active, high selective and potent glucocorticoid receptor (GR) agonist. Flumethasone activates GR to inhibit nuclear factor kappa B (NF-κB)-mediated pro-inflammatory cytokine production (TNF-α, IL-1β) and promotes anti-inflammatory gene expression (IL-10), while also regulating metabolic enzyme activity (tyrosine aminotransferase induction). Flumethasone is promising for research of inflammatory diseases, cancer, and endocrine regulation^[1][2][3][4]. In Vitro:Flumethasone (0-200 nM; 0-24 h) reduces Nrf2 protein levels through glucocorticoid receptor (GCR)-dependent proteasomal degradation in A549 and H460 cells^[1].
Flumethasone (100 nM; 4 h) enhances ubiquitination of Nrf2 in A549 and H460 cells, an effect blocked by GCR knockdown^[1].
In Vivo:Flumethasone (10^-8 to 10^-6 moles/kg, i.p., a single dose) induces a 4- to 10-fold increase in liver tyrosine aminotransferase (TA) activity within 4–6 hours, with prolonged induction compared to hydrocortisone derivatives in adrenalectomized C57BL/6J mice or obese C57BL/6J-ob mutant mice ^[2].