SB242235
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CAS No. | 193746-75-7 | Cat. No. | BCP05992 |
Name | SB242235 | ||
Synonyms | SB-242235;SB 242235; | ||
SMILES | |||
Chemical Name | |||
Formula | C19H20FN5O | M. Wt | 353.39 |
Purity | 98% | Storage | Store at 4-8°C |
Description | in vitro: SB 242235 inhibited intracellular p38 activity, human chondrocytes were treated with different doses of SB 242235 prior to stimulation with IL-1_ for 15 min. MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate. SB 242235 dose-dependently inhibited the activation of MAPKAP K2 with an IC50 of 1.0 uM . in vivo: SB-242235 demonstrates generally favourable pharmacokinetic properties in all species examined(including rat, dog and monkey). Systemic plasma clearance was high in rat, but in the non-rodent species SB-242235 demonstrated low to moderate clearance with plasma half-lives > 4h. Oral bioavailability in each preclinical species was high. In rat and monkey, SB-242235 demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses .In the skin of SKH-1 hairless mice, SB242235, prior to UVB irradiation, blocked activation of the p38 MAPK casca |
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