2. 疾病领域
  3. 神经系统疾病
  4. 神经退行性疾病
  5. 肌萎缩侧索硬化症
  6. K811

K811 是一种具有口服活性的 ASK1 抑制剂，IC50 为 6 nM。K811 可抑制 SOD1G93A 转基因小鼠腰段脊髓中的胶质细胞激活。K811 可延长肌萎缩侧索硬化症小鼠模型--SOD1G93A 转基因小鼠的生存期。K811 可用于肌萎缩侧索硬化症的相关研究。

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K811

K811 Chemical Structure

CAS No. : 1355228-38-4

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K811 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

K811 is an orally active ASK1 inhibitor with an IC50 of 6 nM. K811 inhibits glial cell activation in the lumbar spinal cord of SOD1G93A transgenic mice. K811 extends the survival of SOD1G93A transgenic mice, a mouse model of amyotrophic lateral sclerosis. K811 can be used in studies related to amyotrophic lateral sclerosis[1].

体外研究
(In Vitro)

K811 (1.0 μM; 30 min) 可抑制 NSC34 运动神经元样细胞中由 H2O2 诱导的 ASK1 活化[1]。
K811 (慢病毒感染 24 小时后添加，孵育至接种后第 9 天) 可保护原代运动神经元免受脊髓培养体系中 SOD1G93A 诱导的死亡，该培养体系源自 E12.5 Hb9-GFP 小鼠胚胎[1]。

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

K811 相关抗体:

Western Blot Analysis[1]

Cell Line: NSC34 motor neuron-like cells
Concentration: 1.0 μM
Incubation Time: 30 min (pre-incubation); 15 min (H2O2 treatment)
Result: Significantly reduced the H2O2-induced activation of endogenous ASK1, as measured by decreased levels of phosphorylated ASK1 via immunoblotting.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax AUC0-24
Mice[1] 30 mg/kg p.o. 1.67 h 1.27 nM/mL 13.8 nM·h/mL
体内研究
(In Vivo)

K811 (100 mg/kg；口服；每日；从 28 周龄开始至实验终点) 可使 SOD1G93A 转基因小鼠的生存期延长 1.06%，抑制脊髓 ASK1 的激活，保护运动神经元并减少胶质细胞激活[1]。

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

Animal Model: B6.Cg-Tg(SOD1G93A)dl1Gur/J (male, started treatment at 28 weeks of age, SOD1G93A transgenic ALS model)[1]
Dosage: 100 mg/kg
Administration: p.o.; daily; from 28 weeks of age until endpoint
Result: Extended average survival time to 268.6 days, a 1.06% improvement compared to placebo.
Caused a considerable decrease in ASK1 activation in the spinal cord.
Increased the number of motor neurons in one side of the lumbar spinal cord significantly compared to placebo.
Decreased numbers of glial fibrillary acidic protein (GFAP)-positive astrocytes and ionized calcium binding adaptor molecule 1 (Iba1)-positive microglia markedly in the lumbar spinal cord compared to placebo.
分子量

510.54

Formula

C29H26N4O5
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

K811 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

K8111355228-38-4K 811K-811spinal cord cultureslumbar spinal cordprimary motor neuronsASK1NSC34 motor neuron-like cellsamyotrophic lateral sclerosisSOD1G93A transgenic miceE12.5 Hb9-GFP mouse embryosInhibitorinhibitorinhibit

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