| Bioactivity | Keap1-Nrf2-IN-11 (compound 6k) is a Keap1-Nrf2 inhibitor with KD2 value of 0.21 nM. Keap1-Nrf2-IN-11 inhibits the productions of ROS and NO and the expression of TNF-α. Keap1-Nrf2-IN-11 relieves inflammations by increasing the Nrf2 nuclear translocation. Keap1-Nrf2-IN-11 can be used for anti-inflammatory research[1]. |
| Invitro | Keap1-Nrf2-IN-11 (compound 6k) (10 μΜ) suppresses the production of ROS and NO and inhibits the concentration of proinflammatory cytokine TNF-α in LPS-induced murine peritoneal macrophage model[1]. |
| In Vivo | Keap1-Nrf2-IN-11 (compound 6k) (5-10 mg/kg; i.p.; ALI mouse model) has anti-inflammatory activity in vivo[1].Keap1-Nrf2-IN-11 (compound 6k) (5 mg/kg; i.v.; SD rats) has the half time (T1/2), the clearance rate (CL) and apparent distribution volume (V) were 4.31 h, 5.57 mL/min/kg and 959 L/kg, respectively[1].Keap1-Nrf2-IN-11 (compound 6k) (5 mg/kg; i.p.; ALI mouse model) has the half time (T1/2), maximum plasma concentration (Cmax), area under curve (AUC) and oral bioavailability (F) were 10.92 h, 707 ng/mL, 3702 ng•h/mL and 19.86%, respectively[1]. Animal Model: |
| Name | Keap1-Nrf2-IN-11 |
| Formula | C36H43N7O8S2 |
| Molar Mass | 765.90 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Liu G, et al. Crystallography-Guided Optimizations of the Keap1-Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides. J Med Chem. 2022 Jun 23;65(12):8289-8302. |