biological activity | SD 0006 (SD-06) is an orally effective, selective, ATP competitive, and effective diarylpyrazole inhibitor of p38α MAPK with an IC50 value of 110 nM. |
target | IC50: 110 nM (p38 MAPK). |
in vitro study | SD 0006 clearly inhibits p38α as shown by the dose-dependent inhibition of phosphorylation of its endogenous Hsp27 substrate. |
in vivo study | SD 0006 (0-30 mg/kg) may be an effective alternative to steroids and biologics for RA therapy. SD0006 (3.75, 7.5 and 15 mg/kg; p.o.; B. I. d.) is highly effective in attenuating SCW-induced inflammation as shown by the pose-dependent inhibition of paw swelling. Animal Model: 8- to 12-week-old DBA/1 MICE. Dosage: 3.75, 7.5 and 15 mg/kg. Administration: Orally two daily. Result: inhibited the transcription of several inflammatory mediators to prevent joint swelling and bone destruction and to preserve bone density. |
Animal Model:
| 8- to 12-week-old DBA/1 mice. |
Dosage:
| 3.75, 7.5 and 15 mg/kg. |
Administration:
| Orally twice daily. |
Result:
| Inhibited the transcription of several inflammatory mediators to prevent joint swelling and bone destruction and to preserve bone density. |