Keap1-Nrf2-IN-11 (Compound 6k), a potent Keap1-Nrf2 inhibitor, exhibits a dissociation constant (KD) of 0.21 nM. It hampers the production of reactive oxygen species (ROS) and nitric oxide (NO), as well as the expression of tumor necrosis factor-alpha (TNF-α). By promoting Nrf2 nuclear translocation, it mitigates inflammation and is utilized in anti-inflammatory studies [1].

Keap1-Nrf2-IN-11 (compound 6k) at 10 μΜ significantly inhibits ROS and NO production and reduces proinflammatory cytokine TNF-α levels in an LPS-induced murine peritoneal macrophage model [1].

Keap1-Nrf2-IN-11 (compound 6k) demonstrates anti-inflammatory effects in vivo at dosages of 5-10 mg/kg when administered intraperitoneally in an ALI mouse model. Pharmacokinetic parameters in SD rats, following a 5 mg/kg intravenous dose, show a half-life (T1/2) of 4.31 hours, clearance (CL) of 5.57 mL/min/kg, and an apparent distribution volume (V) of 959 L/kg. In the ALI mouse model with a 5 mg/kg intraperitoneal dose, compound 6k presents a half-life (T1/2) of 10.92 hours, a maximum plasma concentration (Cmax) of 707 ng/mL, an area under the curve (AUC) of 3702 ng•h/mL, and an oral bioavailability (F) of 19.86%.