R1487 Hydrochloride is an orally available, selective and potent inhibitor of mitogen-activated protein kinase (p38α) for the study of metabolic diseases.

IL-1β:200 nM, p38α:0.2 nM (Kd), p38α:10 nM, p38β:29 nM (Kd)

R1487 Hydrochloride is a highly potent and selective inhibitor of p38α with Kd values of 0.2 nM for p38α and 29 nM for p38β. R1487 Hydrochloride has an IC50 value of 10 nM for inhibition of p38α and 200 nM for inhibition of TNFα-induced IL-1β production. R1487 Hydrochloride inhibited p38α with an IC50 value of 10 nM and TNFα-induced IL-1β production with an IC50 value of 200 nM.
R1487 Hydrochloride was able to inhibit TNFα production in a human monocyte cell line (THP-1) and effectively inhibited LPS-induced IL-1β production in human whole blood samples. [1]

After oral administration of R1487 Hydrochloride, its serum levels of TNFα and IL-1β showed significant dose-dependent inhibition.
At a dose of 10 mg/kg orally, the bioavailability of R1487 Hydrochloride in monkeys, mice and dogs reached 51.6%, 29.3% and 10.3%, respectively. [1]