2. NF-κB
  3. Keap1-Nrf2
  4. Keap1-Nrf2-IN-28

Keap1-Nrf2-IN-28 (SG16) 是一种具有口服活性的 Keap1-Nrf2 抑制剂。 Keap1-Nrf2-IN-28 表现出抗氧化能力，诱导 Nrf2、HO-1、GCLM 和 Akr1c1 表达上调。 Keap1-Nrf2-IN-28 可减弱 APAP (HY-66005) 诱导的急性肝损伤。

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Keap1-Nrf2-IN-28 Chemical Structure

Keap1-Nrf2-IN-28 Chemical Structure

CAS No. : 3075750-60-3

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Keap1-Nrf2-IN-28 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Keap1-Nrf2-IN-28 (SG16) is an orally active Keap1-Nrf2 inhibitor. Keap1-Nrf2-IN-28 shows antioxidant capability and induces the upregulation of Nrf2, HO-1, GCLM, and Akr1c1. Keap1-Nrf2-IN-28 attenuates APAP (HY-66005)-induced acute liver injury[1].

体外研究
(In Vitro)

Keap1-Nrf2-IN-28 (Compound SG16) (10 μM，16 小时) 可诱导 AML12 细胞中 HO-1 表达显著增加 10.7 倍，表明其具有 Nrf2 诱导活性[1]。
Keap1-Nrf2-IN-28 (0-10 μM，16 小时) 可上调 AML12 细胞中 HO-1、GCLM 和 Akr1c1 的 mRNA 表达以及 Nrf2、HO-1 和 GCLM 的蛋白表达[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Keap1-Nrf2-IN-28 相关抗体:

RT-PCR[1]

Cell Line: AML12 cells
Concentration: 0.5, 2.5, 5, 10 μM
Incubation Time: 16 h
Result: Induced significant upregulation of HO-1, GCLM, and Akr1c1 expression by 3.4-, 2.3-, and 1.8-fold at 10 μM, respectively.
Dose-dependently increased mRNA level of HO-1, GCLM and Akr1c1.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. AUC0-inf 4726 ng·h/mL
Rat 10 mg/kg p.o. AUC0-inf 8061 ng·h/mL
Rat 1 mg/kg i.v. AUC0-t 3869 ng·h/mL
Rat 10 mg/kg p.o. AUC0-t 7689 ng·h/mL
Rat 1 mg/kg i.v. Cmax 1050 ng/mL
Rat 10 mg/kg p.o. Cmax 1296 ng/mL
Rat 1 mg/kg i.v. T1/2 5.45 hr
Rat 10 mg/kg p.o. T1/2 3.47 hr
Rat 1 mg/kg i.v. Tmax 0.17 hr
Rat 10 mg/kg p.o. Tmax 1.50 hr
Rat 1 mg/kg i.v. CL 20 mL/min/kg
体内研究
(In Vivo)

Keap1-Nrf2-IN-28 (Compound SG16) (12.5 或 25 mg/kg，腹腔注射) 可保护小鼠免受 APAP (HY-66005) 诱发的急性肝损伤 (ALI)[1]。
Keap1-Nrf2-IN-28 (25 mg/kg，腹腔注射) 对 Nrf2 基因敲除小鼠无肝脏保护作用[1]。
Keap1-Nrf2-IN-28 (25 mg/kg，腹腔注射) 在 C57BL/6J 小鼠中表现出良好的生物相容性，且未检测到器官毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: APAP (370 mg/kg, i.p.)-induced acute liver injury (ALI) C57BL/6 mice model[1]
Dosage: 12.5 or 25 mg/kg
Administration: i.p., 1 h following APAP injection, and then samples were collected 12 h later.
Result: Increased both GCLM and HO-1 (100-fold at a dose of 25 mg/kg) mRNA levels in liver tissue than those of negative control (NC) group.
Promoted the nuclear translocation of Nrf2 in liver tissue.
Disrupted the binding between Keap1 and Nrf2 (Co-IP assay).
Significantly reduced ALT/AST levels and attenuated the APAP-conducted elevation of CAT and NO concentrations.
Decreased pathological damage and cell apoptosis in HE staining and TUNEL test.
Lowered liver IL-6 and TNFα levels increased by APAP.
分子量

425.43

Formula

C22H16FNO5S
CAS 号
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.
纯度 & 产品资料
参考文献

Keap1-Nrf2-IN-28 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Keap1-Nrf2-IN-283075750-60-3Keap1-Nrf2AML12 cellsAPAP-induced ALI In vivoInhibitorinhibitorinhibit

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