RO31-8220甲磺酸盐
RO31-8220甲磺酸盐 性质
| 密度 | 1.42±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | H2O: 7.3 mg/mL |
| 酸度系数(pKa) | 7.90±0.60(Predicted) |
| 形态 | 固体 |
| 颜色 | 橙色至红色 |
RO31-8220甲磺酸盐 用途与合成方法
|
PKC-α 5 nM (IC 50 ) |
PKC-βII 14 nM (IC 50 ) |
PKC-βI 24 nM (IC 50 ) |
PKC-ε 24 nM (IC 50 ) |
PKC-γ 27 nM (IC 50 ) |
Rat Brain PKC 23 nM (IC 50 ) |
MAPKAP-K1b 3 nM (IC 50 ) |
MSK1 8 nM (IC 50 ) |
S6K1 15 nM (IC 50 ) |
GSK3β 38 nM (IC 50 ) |
Ro 31-8220 is a potent PKC inhibitor, with IC 50 s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC 50 s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Moreover, Ro 31-8220 directly suppresses voltage-dependent Na + channels. Ro 31-8220 (1 μM) is neuroprotective against paraoxon-induced neuronal cell death in cerebellar granule neurons, blocks paraoxon-induced caspase-3 activity, and reduces the paraoxon-induced increase in phospho-PKC pan levels.
Ro 31-8220 (6 mg/kg/d, s.c.) is well tolerated, and has half-life of 5.7 hours in mice. Ro 31-8220-treated MLP −/− mice show a dramatic rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change.
RO31-8220甲磺酸盐 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-13866 | 5 mg | 801 | ||
| 2024-11-08 | HY-13866 | 1G,10G,100G,1KG | 125314-64-9 | 10 mg | 1244 |
