中文名 | Ro 31-8220 |
英文名 | Ro 31-8220 |
别名 | RO31-8220甲磺酸盐是广谱PKC抑制剂 |
英文别名 | Ro 31-8220 RO-31-8220 RO 31-8220 MESYLATE RO 31-8220 METHANESULFONATE BISINDOLYLMALEIMIDE IX METHANESULFONATE BISINDOYLMALEIMIDINE IX METHANESULFONATE 3-[1-3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL) MALEIMIDE 3-[1-[3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL)MALEIMIDE METHANESULFONATE 3-[3-[2,5-DIHYDRO-4-(1-METHYL-1H-INDOL-3-YL)-2,5-DIOXO-1H-PYRROL-3-YL]-1H-INDOL-1-YL]PROPYL CARBAMIMIDOTHIOIC ACID ESTER MESYLATE |
CAS | 125314-64-9 |
化学式 | C25H23N5O2S |
分子量 | 457.55 |
密度 | 1.42±0.1 g/cm3(Predicted) |
溶解度 | H2O: 7.3mg/ml |
酸度系数 | 7.90±0.60(Predicted) |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | orange to red |
体外研究 | 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. |
体内研究 | 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. |
WGK Germany | 3 |
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