IRAK4-IN-28

CAS: 2952532-92-0 F: C27H31N9O3 W: 529.59

IRAK4-IN-28 (compound 42) is an orally active IRAK4 inhibitor (IC50=8.9 nM). IRAK4-IN-28 has binding affinity for IRAK4

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Bioactivity	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].
Target	IC50:8.9 nM (IRAK4), IC50:>30 nM (hERG), Kd:0.58 nM (IRAK4), Kd:140 nM (IRAK1)
Invitro	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]。 Cell Viability Assay[1] Cell Line:
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]。 Animal Model:
Name	IRAK4-IN-28
CAS	2952532-92-0
Formula	C27H31N9O3
Molar Mass	529.59
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Yongjin Hao, et al. Design, synthesis, evaluation and optimization of potent IRAK4 inhibitors alleviating production of inflammatory cytokines in LPS-induced SIRS model. Bioorg Chem. 2023 , 137:106584.

(BHQ-3)-OSu hexafluorophosphate