2. Immunology/Inflammation
  3. IRAK
  4. IRAK4-IN-28

IRAK4-IN-28 (compound 42) 是一种口服活性的 IRAK4 抑制剂 (ICIC50=8.9 nM)。IRAK4-IN-28 对 IRAK4 具有结合亲和力，Kd 为 0.58 nM。IRAK4-IN-28 可用于炎症和自身免疫性疾病的研究。

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IRAK4-IN-28 Chemical Structure

IRAK4-IN-28 Chemical Structure

CAS No. : 2952532-92-0

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IRAK4-IN-28 相关抗体

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IRAK1 IRAK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IRAK4-IN-28 (compound 42) is an orally active IRAK4 inhibitor (IC50=8.9 nM). IRAK4-IN-28 has binding affinity for IRAK4 with a Kd of 0.58 nM. IRAK4-IN-28 can be used in the research of inflammation and autoimmune diseases[1].

IC50 & Target

IC50:8.9 nM (IRAK4)[1], IC50:>30 nM (hERG)[1], Kd:0.58 nM (IRAK4)[1], Kd:140 nM (IRAK1)[1]
体外研究
(In Vitro)

IRAK4-IN-28 对细胞色素 P450 酶 CYP1A2、CYP2D6、CYP3A4 和 hERG 没有抑制作用，这意味着良好的安全性和“药物相似性”特性[1]。
IRAK4-IN-28 抑制 CYP2C9、CYP2C19，IC50 分别为 12 μM 和 2.7 μM[1]。
IRAK4-IN-28 在人和大鼠中具有较高的血浆蛋白结合率（分别为 99.8 和 97.2）[1]。
IRAK4-IN-28 (1 h) 在 mRNA 和蛋白水平抑制 LPS 诱导的 TNF-α 和 IL-6 表达，且呈剂量依赖性[1]。

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

IRAK4-IN-28 相关抗体:

Cell Viability Assay[1]

Cell Line: iBMDM cell
Concentration: 0-33 μM
Incubation Time: 1 h
Result: Reduced mRNA levels and protein levels of TNF-α and IL-6 in mouse iBMDM cells.
体内研究
(In Vivo)

IRAK4-IN-28 (compound 42) 在大鼠模型中有良好的药代动力学数据[1]。
IRAK4-IN-28 具有口服生物活性，利用率为 68%[1]。
IRAK4-IN-28 (50 or 100 mg/ml, single dose, oral) 在小鼠模型中显著减少了 LPS 诱导的细胞因子 TNF-α 和 IL-6 的释放[1]。

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

Animal Model: LPS-stimulated female C57BL/6 mice[1]
Dosage: 50 or 100 mg/ml, single dose; 1 h prior to 1 mg/kg LPS administration by intraperitoneal injection
Administration: Oral gavage (p.o.)
Result: Inhibited cytokine TNF-α and IL-6 in a dose-dependent manner in an LPS-stimulated mouse model.
分子量

529.59

Formula

C27H31N9O3
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

IRAK4-IN-28 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • 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:

IRAK4-IN-282952532-92-0IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseInhibitorinhibitorinhibit

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产品名称：
IRAK4-IN-28
目录号：
HY-155132
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