2. NF-κB Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. Keap1-Nrf2 NO Synthase ROS Kinase
  4. Keap1-Nrf2-IN-11

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。

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Keap1-Nrf2-IN-11 Chemical Structure

Keap1-Nrf2-IN-11 Chemical Structure

CAS No. : 2796292-75-4

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Keap1-Nrf2-IN-11 相关抗体

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nNOS iNOS eNOS

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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].

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

Keap1-Nrf2-IN-11 相关抗体:
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 ng•h/mL and 19.86%, respectively[1].

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

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
分子量

765.90

Formula

C36H43N7O8S2
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-11 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-112796292-75-4Keap1-Nrf2NO SynthaseROS KinaseNitric oxide synthasesNOSanti-inflammatoryNrf2 nuclear translocationROSNOInhibitorinhibitorinhibit

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