IRAK4-IN-21 (化合物 17) 是一种口服有效的和具有选择性的强效IRAK4抑制剂，其对IRAK4和TAK1的IC50值分别为 5 和 56 nM。IRAK4-IN-21 能够有效抑制 IL-23 的产生 (IC50=0.17 μM)，可用于自身免疫性疾病，如斑块状银屑病和银屑病关节炎的研究。

IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC 50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production ( IC 50 =0.17 μM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis [1].

IRAK4-IN-21 (a 4-fold serial dilution from 10 μM; 1 h) decreases the levels of IL-23 (in THP-1 and DC cells), IL-6 (in HUVEC cells) and MIP-1β (in human whole blood) [1]. Cell Viability Assay [1] Cell Line: THP-1, DC cells (are primed with IFN-γ) Concentration: 10 μM (a 4-fold serial dilution from 10 μM) Incubation Time: 1 h (pre-incubate) Result: Inhibited the levels of IL-23 in the supernatant of THP-1 and DC cells with IC 50 of 0.17 and 0.51 μM, respectively. Cell Viability Assay [1] Cell Line: HUVEC cells (IL-1β-stimulated) Concentration: 10 μM (a 4-fold serial dilution from 10 μM) Incubation Time: 1 h (pre-incubate) Result: Inhibited the level of IL-6 in the supernatant of HUVEC cells with an IC 50 of 0.20 μM. Cell Viability Assay [1] Cell Line: Human whole blood (IL-1β-stimulated) Concentration: 10 μM (a 4-fold serial dilution from 10 μM) Incubation Time: 1 h (pre-incubate) Result: Inhibited the level of MIP-1β in the human whole blood with an IC 50 of 0.47 μM.

IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production [1]. Animal Model: BALB/c mice (acute mouse model; IL-1β-stimulated) [1]. Dosage: 75 mg/kg Administration: Oral administration; single (pre-treat). Result: Showed 54% inhibition of IL-6, plasma concentrations was 2877 ng/mL at 0.5 h and 496 ng/mL at 2 h.

2170694-04-7

C28H28FN7O2

513.57

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