產(chǎn)品描述: | SL327 inhibits MEK1 and MEK2, with IC50 values of 180 nM and 220 nM, respectively. |
靶點(diǎn): |
MEK1:180 nM (IC50);MEK2:220 nM (IC50);MEK;DNA/RNASynthesis |
體內(nèi)研究: |
SL327, which crosses the blood-brain barrier, is administered intraperitoneally at several concentrations to animals prior to cue and contextual fear conditioning. Administration of SL327 completely blocks contextual fear conditioning and significantly attenuates cue learning when measure 24 hr after training. Animals treated with SL327 exhibit significant attenuation of water maze learning; they take significantly longer to find a hidden platform compared with vehicle-treated controls and also fail to use a selective search strategy during subsequent probe trials in which the platform is removed. Mice are injected with various concentrations of SL327 (10, 30, 50 mg/kg i.p.), and 1 hr later their hippocampi are removed and assayed for activated MAPK. SL327 attenuates phosphorylated MAPK levels in a dose-dependent manner. Administration of 10, 30, or 50 mg/kg SL327 significantly attenuates p42 phospho-MAPK levels (F=20.90, P<0.0001;10 mg/kg SL327 vs. vehicle, P<0.05, and 30 and 50 mg/kg SL327 vs. vehicle, P<0.001). Injection with 30 or 50 mg/kg SL327 also significantly reduces p44 phospho-MAPK levels (F=5.627, P<0.005;30 mg/kg vs. vehicle, P<0.05, and 50 mg/kg SL327 vs. vehicle, P<0.01) |
參考文獻(xiàn): |
1. Cheng Y, et al. Current Development Status of MEK Inhibitors. Molecules. 2017 Sep 26;22(10). pii: E1551. 2. Selcher JC, et al. A necessity for MAP kinase activation in mammalian spatial learning. Learn Mem. 1999 Sep-Oct;6(5):478-90. |
溶解性: |
DMSO : 68 mg/mL (202.77 mM; Need ultrasonic) Ethanol : 0.1 mg/mL (0.30 mM; Need ultrasonic and warming) |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.982 ml |
14.91 ml |
29.82 ml |
5 mM |
0.596 ml |
2.982 ml |
5.964 ml |
10 mM |
0.298 ml |
1.491 ml |
2.982 ml |
50 mM |
0.06 ml |
0.298 ml |
0.596 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |