Molecular Formula | C20H20ClN5O2 |
Molar Mass | 397.86 |
Density | 1.367 |
Boling Point | 652.6±55.0 °C(Predicted) |
Solubility | DMSO: ≥ 29 mg/mL |
pKa | 9.39±0.50(Predicted) |
Storage Condition | 2-8°C |
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 dose-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 twice daily. Result: Inhibited the transcription of several inflammatory mediators to prevent joint swelling and bone destruction and to preserve bone density. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.513 ml | 12.567 ml | 25.135 ml |
5 mM | 0.503 ml | 2.513 ml | 5.027 ml |
10 mM | 0.251 ml | 1.257 ml | 2.513 ml |
5 mM | 0.05 ml | 0.251 ml | 0.503 ml |
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. |