IRAK4-IN-1 是白细胞介素-1 受体相关激酶 4 抑制剂(IC50:7 nM)。

IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.

The in vitro metabolic stability profiles of IRAK4-IN-1 is measured, with EC50 of 2300 nM for the rat whole blood (RWB)

Oral pharmacokinetic studies of IRAK4-IN-1 show it to have high bioavailability of 73% and low plasma clearance (Clp=22 mL/min/kg) leading to a reasonable half-life of 1.3 h.

In the TLR driven in vivo model, female Lewis rats are dosed with either vehicle or IRAK4-IN-1 (Compound 23; 3, 10, 30, and 100 mg/kg; p.o.) dosed at 1 h prior to stimulation with Resiquimod, R848 (5 mg/kg, IP). At 1.5 h post R848 stimulation, blood samples are obtained from the animals and cytokine levels are measured.

1820787-94-7

C19H23N5O

337.427

DMSO:14.29 mg/mL (42.35 mM),Need ultrasonic
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years