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IRAK4-IN-1

Names

[ CAS No. ]:
1820787-94-7

[ Name ]:
IRAK4-IN-1

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> IRAK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IRAK
Research Areas >> Inflammation/Immunology

[Target]

IC50: 7 nM (IRAK4)[1]


[In Vitro]

The in vitro metabolic stability profiles of IRAK4-IN-1 (Compound 23) is measured, with EC50 of 2300 nM for the rat whole blood (RWB) [1].

[In Vivo]

Oral pharmacokinetic studies of IRAK4-IN-1 (Compound 23) 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[1].

[Animal admin]

Rats[1] 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.

[References]

[1]. Smith GF, et al. Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2721-2726.


[Related Small Molecules]

IRAK-1-4 Inhibitor I | PF06650833 | CA-4948 | ginsenoside Rb1 | IRAK inhibitor 1 | IRAK inhibitor 4 | IRAK inhibitor 2 | IRAK inhibitor 3 | IRAK inhibitor 6

Chemical & Physical Properties

[ Molecular Formula ]:
C19H23N5O

[ Molecular Weight ]:
337.42

[ Appearance of Characters ]:
off white solid

[ Storage condition ]:
-20℃

Related Compounds