Keap1-Nrf2-IN-11 是一种Keap1-Nrf2抑制剂，其KD2值为 0.21 nM。Keap1-Nrf2-IN-11 抑制 ROS 和 NO 的产生以及 TNF-α 的表达。Keap1-Nrf2-IN-11 通过增加 Nrf2 核易位来缓解炎症。Keap1-Nrf2-IN-11 可用于抗炎研究。
| 生物活性 | Keap1-Nrf2-IN-11 (compound 6k) is aKeap1-Nrf2inhibitor withKD2value 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]. |
体外研究
(In Vitro) | 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].
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体内研究
(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 ngoh/mL and 19.86%, respectively[1].
| Animal Model: | ALI mouse model[1] | | 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[1] | | 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[1] | | Dosage: | 5 and 20 mg/kg | | Administration: | Intraperitoneal injection and oral gavage | | Result: | 1.19|
| Administration | i.g. (20 mg/kg) | i.v. (5 mg/kg) | | Tmax(h) | 1.38 | 0.72 | | Tmax(h) | 10.92 | 4.31 | | Cmax(ng/mL) | 707.62 | 2631.69 | | AUC0-24(ng·h/mL) | 3061.55 | 4561.21 | | AUC0-∞(ng·h/mL)CL (mL/min/kg) | 3702.22 | 4799.24 | | CL (L/h/kg) | 6503.05 | 5.57 | | V (L/kg) | 114127.5 | 959.54 | | MRT0-24(h) | 6.71 | 4.64 | | MRT0-∞(h) | 13.97 | 5.94 | | F % | 19.86 | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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