IRAK4-IN-19 是一种有效的白介素 1 受体相关激酶 4 (IRAK4)抑制剂，IC50为 4.3 nM。IRAK4-IN-19 可抑制 THP 和 DC 细胞中 LPS 诱导的 IL23 产生，阻止关节炎模型大鼠的关节炎发展。IRAK4-IN-19 可用于关节炎疾病的研究。

IRAK4-IN-19 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC 50 value of 4.3 nM. IRAK4-IN-19 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-19 can be used for researching arthritis disease [1].

IRAK4-IN-19 (compound 39) has inhibitory activity against LPS-induced IL23 in THP and DC with IC 50 s of 0.23 and 0.22 μM, respectively [1].

IRAK4-IN-19 (30 mg/kg; twice daily for 21 days) completely stops arthritis development in arthritis rats at 30 mg/kg [1]. IRAK4-IN-19 (1 mg/kg for IV, 5 mg/kg for PO, single dosage) exhibits a favorable pharmacokinetics profile [1]. IRAK4-IN-19 (5, 15, 45 and 75 mg/kg) exhibits good efficacy in an acute mouse model for the IL-1β induced IL-6 expression, with 64% inhibition at 75 mg/kg dose, 37% inhibition at 45 mg/kg dose, 16% inhibition at 15 mg/kg dose and 9% inhibition at 5 mg/kg [1]. Animal Model: Rats [1] Dosage: 30 mg/kg Administration: twice daily for 21 days Result: Completely stopped arthritis development in arthritis rats at 30 mg/kg. Animal Model: Rats [1] Dosage: 1 mg/kg, 5 mg/kg Administration: IV and PO, single dosage Result: Exhibited a favorable pharmacokinetics profile with a clearance of 6 mL/min/kg and oral bioavailability of 43%.

C25H26F2N8O

492.52

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years