SB 242235
Modify Date: 2026-06-30 11:36:53
SB 242235 structure
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Common Name | SB 242235 | ||
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| CAS Number | 193746-75-7 | Molecular Weight | 353.393 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 568.4±60.0 °C at 760 mmHg | |
| Molecular Formula | C19H20FN5O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 297.5±32.9 °C | |
Use of SB 242235SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 uM.IC50 Value: 1.0 uM [1]Target: p38 MAPKin 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 [1].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 [2].In the skin of SKH-1 hairless mice, SB242235, prior to UVB irradiation, blocked activation of the p38 MAPK cascade, and abolished MAPKAPK-2 kinase activity and phosphorylation of HSP27. Moreover, SB242235 inhibited expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2 [3]. The preclinical pharmacokinetics of SB-242235 have been described previously. The present studies were conducted to describe the in vitro metabolic rates and routes of SB-242235 metabolism, to characterize its in vivo preclinical metabolism, and to use these data to aid in the prediction of the pharmacokinetic behaviour of SB-242235 in man [4]. |
| Name | 4-[5-(4-fluorophenyl)-3-piperidin-4-ylimidazol-4-yl]-2-methoxypyrimidine |
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| Synonym | More Synonyms |
| Description | SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 uM.IC50 Value: 1.0 uM [1]Target: p38 MAPKin 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 [1].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 [2].In the skin of SKH-1 hairless mice, SB242235, prior to UVB irradiation, blocked activation of the p38 MAPK cascade, and abolished MAPKAPK-2 kinase activity and phosphorylation of HSP27. Moreover, SB242235 inhibited expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2 [3]. The preclinical pharmacokinetics of SB-242235 have been described previously. The present studies were conducted to describe the in vitro metabolic rates and routes of SB-242235 metabolism, to characterize its in vivo preclinical metabolism, and to use these data to aid in the prediction of the pharmacokinetic behaviour of SB-242235 in man [4]. |
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| Related Catalog | |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 568.4±60.0 °C at 760 mmHg |
| Molecular Formula | C19H20FN5O |
| Molecular Weight | 353.393 |
| Flash Point | 297.5±32.9 °C |
| Exact Mass | 353.165192 |
| PSA | 64.86000 |
| LogP | 3.01 |
| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
| Index of Refraction | 1.662 |
| InChIKey | PDTYLGXVBIWRIM-UHFFFAOYSA-N |
| SMILES | COc1nccc(-c2c(-c3ccc(F)cc3)ncn2C2CCNCC2)n1 |
| Storage condition | 2-8℃ |
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| 4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxypyrimidine |
| Kinome_3169 |
| HMS3244I17 |
| HMS3244I18 |
| HMS3244J17 |
| 4-[4-(4-fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl]-2-methoxypyrimidine |
| 4-(4-(4-fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl)-2-methoxypyrimidine |
| SB 242235 |