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编 号:F747906
分子式:C30H29NO8S
分子量:563.62
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生物活性:
Keap1-Nrf2-IN-14 (compound 20c) is a KEAP1-NRF2 inhibitor that effectively disrupts the KEAP1-NRF2 interaction (IC50=75 nM) with a Kd value of 24 nM for KEAP1. Keap1-Nrf2-IN-14 induces the expression of NRF2 target genes and enhances the downstream antioxidant and anti-inflammatory activities. Keap1-Nrf2-IN-14 can be used in the study of oxidative stress-related inflammation.

体内研究:
Keap1-Nrf2-IN-14 (10 mg/kg; i.p.; single daily for 3 days) reduces the LPS-induced production of the proinflammatory factors in vivo.Keap1-Nrf2-IN-14 (1 mg/kg; i.v.; single) shows half-life of 1.72 h in vivo.Animal Model:Female C57BL/6 mice (18-22 g; LPS-induced inflammation model).
Dosage:10 mg/kg
Administration:Intraperitoneal injection; single daily for 3 days.
Result:Diminished LPS-induced inflammatory response in vivo.
Animal Model:Female C57BL/6 mice (18-22 g; LPS-induced inflammation model).
Dosage:1 mg/kg
Administration:Intravenous injection; single.
Result:Led to half-life of 1.72 h.

体外研究:
Keap1-Nrf2-IN-14 effectively activated NRF2-ARE regulated cytoprotective defense system in both concentration- and time- dependent manner in RAW264.7 cells.Keap1-Nrf2-IN-14 (1, 10 μM; 12 h) enhanced the antioxidant capacity in macrophage RAW 264.7 cells.Keap1-Nrf2-IN-14 (1, 10 μM; 12 h) attenuates LPS-induced production of inflammation factors in RAW 264.7 cells.Keap1-Nrf2-IN-14 shows high metabolic stability (in co-incubation with rat liver microsomes with half-life of 10.5 h), and have no CYP inhibition on 1A2, 2C9, 2C19, 2D6 and 3A4 when at 10 μM.
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