IRAK4-IN-18 是一种有效的白介素 1 受体相关激酶 4 (IRAK4)抑制剂，IC50为 15 nM。IRAK4-IN-18 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-18 可用于关节炎疾病的研究。

IRAK4-IN-18 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC 50 value of 15 nM. IRAK4-IN-18 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-18 can be used for researching arthritis disease [1].

IRAK4-IN-18 (compound 33) has inhibitory activity against LPS-induced IL23 in THP and DC with IC 50 s of 0.25 and 0.14 μM, respectively [1].

IRAK4-IN-18 (5, 10 and 20 mg/kg; twice daily for 21 days) exhibits good efficacy in a mouse model for the inhibition of IL-6 production induced by IL-1β, and completely stops arthritis development in arthritis rats at 30 mg/kg [1]. IRAK4-IN-18 (1 mg/kg for IV, 5 mg/kg for PO, single dosage) exhibits a favorable pharmacokinetics profile with a clearance of 53 mL/min/kg and oral bioavailability of 38% [1]. Animal Model: Collagen-induced arthritis (CIA) rat models [1] Dosage: 5, 10 and 20 mg/kg Administration: twice daily for 21 days Result: Completely stopped arthritis development based on hind paw clinical scores at 30 mg/kg dose, twice daily, and effectively decreased disease progression with 97% inhibition at 20 mg/kg dose, 56% inhibition at 10 mg/kg dose and 30% inhibition at 5 mg/kg dose.

C24H25FN6O3

464.49

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