3-[N-(2-Hydroxyacetyl)-4-piperidyl]-4-(4-pyrimidinyl)-5-(4-chlorophenyl)pyrazole

Definition

ChEBI: SD-06 is a member of the class of pyrazoles that is 1H-pyrazole in which the hydrogens at positions 3, 4, and 5 are replaced by N-(hydroxyacetyl)piperidin-4-yl, pyrimidin-4-yl and p-chlorophenyl groups, respectively. It is a member of pyrazoles, a member of pyrimidines, a N-acylpiperidine, a member of monochlorobenzenes and a primary alcohol.

Biological Activity

SD 0006 (SD-06) is an orally potent, selective, ATP-competitive, and potent diarylpyrazole inhibitor of p38α MAPK with IC50 of 110 nM.

in vitro

SD 0006 clearly inhibits p38α as shown by the dose-dependent inhibition of phosphorylation of its endogenous Hsp27 substrate.

in vivo

SD 0006 (0-30 mg/kg) may be an effective alternative to steroids and biologics for RA therapy.It(3.75, 7.5 and 15 mg/kg; po; bid) is highly effective in attenuating SCW-induced inflammation as shown by the dose-dependent inhibition of paw swelling.