产品
编 号：F756033
分子式：C36H43N7O8S2
分子量：765.9
分子式：C36H43N7O8S2
分子量：765.9
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CAS No: 2796292-75-4
产品详情
生物活性：
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.
体内研究：
Keap1-Nrf2-IN-11 (compound 6k) (5-10 mg/kg; i.p.; ALI mouse model) has anti-inflammatory activity in vivo.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.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.Animal Model:ALI mouse model
Dosage:5, 10 and 20 mg/kg
Administration:Intraperitoneal injection; 30 mins.
Result:Had lower TNF-α, IL-1β and IL-6 levels in BALF in a dose-dependent manner.
Animal Model:ALI mouse model
Dosage:5, 10 and 20 mg/kg
Administration:Intraperitoneal injection; 30 mins.
Result:Induced the Nrf2 nuclear accumulation in lung tissue cells by decreasing the cytosolic Nrf2 and increasing the nuclear Nrf2 in a dose?response manner.
Animal Model:SD rats
Dosage:5 and 20 mg/kg
Administration:Intraperitoneal injection and oral gavage
Result:1.19 Administrationi.g. (20 mg/kg)i.v. (5 mg/kg)
Tmax (h)1.380.72
Tmax (h)10.924.31
Cmax (ng/mL)707.622631.69
AUC0-24 (ng·h/mL)3061.554561.21
AUC0-∞ (ng·h/mL)CL (mL/min/kg)3702.224799.24
CL (L/h/kg)6503.055.57
V (L/kg)114127.5959.54MRT0-24 (h)6.714.64
MRT0-∞ (h)13.975.94
F %19.86
体外研究：
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.
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.
体内研究：
Keap1-Nrf2-IN-11 (compound 6k) (5-10 mg/kg; i.p.; ALI mouse model) has anti-inflammatory activity in vivo.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.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.Animal Model:ALI mouse model
Dosage:5, 10 and 20 mg/kg
Administration:Intraperitoneal injection; 30 mins.
Result:Had lower TNF-α, IL-1β and IL-6 levels in BALF in a dose-dependent manner.
Animal Model:ALI mouse model
Dosage:5, 10 and 20 mg/kg
Administration:Intraperitoneal injection; 30 mins.
Result:Induced the Nrf2 nuclear accumulation in lung tissue cells by decreasing the cytosolic Nrf2 and increasing the nuclear Nrf2 in a dose?response manner.
Animal Model:SD rats
Dosage:5 and 20 mg/kg
Administration:Intraperitoneal injection and oral gavage
Result:1.19 Administrationi.g. (20 mg/kg)i.v. (5 mg/kg)
Tmax (h)1.380.72
Tmax (h)10.924.31
Cmax (ng/mL)707.622631.69
AUC0-24 (ng·h/mL)3061.554561.21
AUC0-∞ (ng·h/mL)CL (mL/min/kg)3702.224799.24
CL (L/h/kg)6503.055.57
V (L/kg)114127.5959.54MRT0-24 (h)6.714.64
MRT0-∞ (h)13.975.94
F %19.86
体外研究：
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.
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