| Identification | Back Directory | [Name]
SB242235 | [CAS]
193746-75-7 | [Synonyms]
CS-668
SB242235
SB242235 ≥95%
SB-242235; SB242235
4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxypyrimidine
4-(4-(4-Fluorophenyl)-1-(piperidin-4-yl)-1H-iMidazol-5-yl)-2-MethoxypyriMidine
Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy- | [Molecular Formula]
C19H20FN5O | [MDL Number]
MFCD08690575 | [MOL File]
193746-75-7.mol | [Molecular Weight]
353.39 |
| Chemical Properties | Back Directory | [Boiling point ]
568.4±60.0 °C(Predicted) | [density ]
1.34 | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
DMF: 25 mg/ml; DMSO: 20 mg/ml; Ethanol: 30 mg/ml | [form ]
Powder | [pka]
9.91±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0 μM in primary human chondrocytes[1]. | [Biological Activity]
SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 μM in human chondrocytes. | [in vitro]
SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC 50 of 1.0 μM in human chondrocytes stimulated with IL-1β.
SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate.
Western Blot Analysis | Cell Line: | Human chondrocytes | | Concentration: | 0 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM | | Incubation Time: | < td class="col2"> 15 minutes | Result: | Dose-dependently inhibited the activation of MAPKAP K2 with an IC 50 of 1.0 μM. | | [in vivo]
SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation[2].
SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2[2].
SB-242235 is 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 rat and monkey[3].
| Animal Model: | Female SKH-1 hairless mice (4–6 weeks)[2] | | Dosage: | 100 mg/kg | | Administration: | Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation | | Result: | Abolished MAP-KAPK-2 activity and heat shock protein 27 (HSP27) phosphorylation. |
| [target]
IC50: 1.0 μM (p38 MAPK, primary human chondrocytes) | [storage]
Store at -20°C | [References]
[1] Badger, A.M., et al., Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte cultures. Osteoarthritis Cartilage, 2000. 8(6): p. 434-43. DOI:10.1053/joca.1999.0319
[2] Kim AL , et al. Role of p38 MAPK in UVB-induced inflammatory responses in the skin of SKH-1 hairless mice. J Invest Dermatol. 2005 Jun;124(6):1318-25. DOI:10.1111/j.0022-202X.2005.23747.x
[3] Ward, K.W., et al., SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. I: preclinical pharmacokinetics. Xenobiotica, 2002. 32(3): p. 221-33. DOI:10.1080/00498250110100720 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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