SB 242235

小分子

4-[5-(4-fluorophenyl)-3-piperidin-4-ylimidazol-4-yl]-2-methoxypyrimidine | 2-(2-fluorophenylamino)benzoic acid | FT-0734865 | BCP05992 | CB09119 | SB 242235 | DTXSID701026008 | 4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxypyrimidine;

SB 242235

S649694-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC 50 of 1.0 μM in primary 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:IC50: 1.0 μM (p38 MAPK, primary human chondrocytes)

SB-242235 是一种强效的选择性 p38 MAP 激酶抑制剂，在原代人类软骨细胞中的 IC 50 为 1.0u3000μM。

193746-75-7

C19H20FN5O

353.4 g/mol

9863367

COC1=NC=CC(=N1)C2=C(N=CN2C3CCNCC3)C4=CC=C(C=C4)F

4-[5-(4-fluorophenyl)-3-piperidin-4-ylimidazol-4-yl]-2-methoxypyrimidine

1S/C19H20FN5O/c1-26-19-22-11-8-16(24-19)18-17(13-2-4-14(20)5-3-13)23-12-25(18)15-6-9-21-10-7-15/h2-5,8,11-12,15,21H,6-7,9-10H2,1H3

PDTYLGXVBIWRIM-UHFFFAOYSA-N

COC1=NC=CC(=N1)C2=C(N=CN2C3CCNCC3)C4=CC=C(C=C4)F

9863367

193746-75-7

SB 242235;SB-242235;SB242235

DMSO : ≥ 48 mg/mL (135.83 mM)

1

6

4

353.165 Da

353.165 Da

64.900 Ų

26

0

442

0

1

2.1