IRAK4-IN-28 

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].

IC50:8.9 nM (IRAK4)^[1], IC50:>30 nM (hERG)^[1], Kd:0.58 nM (IRAK4)^[1], Kd:140 nM (IRAK1)^[1]

IRAK4-IN-28 (compound 42) has no inhibition on cytochrome P450 enzymes CYP1A2, CYP2D6, CYP3A4, and hERG which means a good safety and ‘drug-likeness’ properties^[1].
IRAK4-IN-28 inhibits CYP2C9, CYP2C19 with IC₅₀ of 12 μM and 2.7 μM, respectively^[1].
IRAK4-IN-28 has high plasma protein binding in human and rat (99.8 an 97.2, respectively)^[1].
IRAK4-IN-28 (1 h) inhibits the LPS (HY-D1056)-induced TNF-α and IL-6 expression at both mRNA and protein levels in a dose-dependent manner^[1].

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

IRAK4-IN-28 (compound 42) has favorable pharmacokinetic properties in the SD rat model^[1].
IRAK4-IN-28 has orally bioactive with 68% availability^[1].
IRAK4-IN-28 (50 or 100 mg/ml, single dose, oral ) significantly reduces LPS-induced TNF-α and IL-6 cytokines release in the mouse model^[1].

Pharmacokinetic Analysis in male SD Rat Model^[1]

大鼠模型中药代动力学分析^[1]

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

529.59

C₂₇H₃₁N₉O₃

2952532-92-0

CN1N=CC(C2=CC=CC(NC(C3=CC(O4)=C(N=C3N5CCN(C6CC6)CC5)N=C4N7CCOCC7)=O)=N2)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]