IRAK4-IN-21

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. In Vitro 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AssayCell 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 AssayCell 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. In Vivo IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c mice (acute mouse model; IL-1β-stimulated) . 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. Form:Solid

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