中文名 | Ro 31-8220 Mesylate |
英文名 | Ro 31-8220 Mesylate |
别名 | RO31-8220 MSOH盐 双吲哚马来酰亚胺 IX 甲烷磺酸盐 3-(3-(4-(1-甲基-1H-吲哚-3-基)-2,5-二氧代-2,5-二氢-1H-吡咯-3-基)-1H-吲哚-1-基)丙基异硫脲甲磺酸盐 |
英文别名 | RO-31-8220 MK-7123, PS-291822 Ro 31-8220 Mesylat Ro 31-8220 Mesylate BisindolylMaleiMide IX Mesylate BISINDOLYLMALEIMIDE IX, METHANESULFONATE BISINDOLYLMALEIMIDE IX METHANESULPHONATE SALT BisindolylMaleiMide IX . Methansulfonate [Ro 31-8220] 3-[1-[3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL)MALEIMIDE |
CAS | 138489-18-6 |
化学式 | C25H23N5O2S |
分子量 | 457.55 |
存储条件 | 2-8°C |
外观 | 红色固体 |
体外研究 | Ro 31-8220 mesylate 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.806 ml | 9.031 ml | 18.062 ml |
5 mM | 0.361 ml | 1.806 ml | 3.612 ml |
10 mM | 0.181 ml | 0.903 ml | 1.806 ml |
5 mM | 0.036 ml | 0.181 ml | 0.361 ml |
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