Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy-

Name	SB 242235
Synonyms	CS-668 SB242235 SB242235 SB-242235 SB 242235 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-
CAS	193746-75-7

Molecular Formula	C19H20FN5O
Molar Mass	353.39
Density	1.34
Boling Point	568.4±60.0 °C(Predicted)
Solubility	DMSO: ≥ 48 mg/mL
pKa	9.91±0.10(Predicted)
Storage Condition	2-8°C(protect from light)
In vitro study	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: 15 minutes Result: Dose-dependently inhibited the activation of MAPKAP K2 with an IC 50 of 1.0 μM.
In vivo study	SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation. SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-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. Animal Model: Female SKH-1 hairless mice (4–6 weeks) 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.

Last Update：2024-01-02 23:10:35

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CAS: 193746-75-7
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Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy- Request for Quotation