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Ro 31-8220  

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产品描述：基本信息 产品编号：R10288 产品名称：Ro 31-8220 CAS: 125314-64-9   储存条件 粉末 -20℃ 四年 分子式： C25H23N5O2S 溶于液体 -80℃ 一年 分子量： 457.55     化学名：      Solubility (25°C)   体外 DMSO 100mg/mL (180.61mM) Ethanol Insoluble Water Insoluble 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.8062mL 9.0310mL 18.0620mL 5mM 0.3612mL 1.8062mL 3.6124mL 10mM 0.1806mL 0.9031mL 1.8062 mL 50mM 0.0361mL 0.1806mL 0.3612mL   生物活性 产品描述 一种有效的 PKC 抑制剂，对 PKCα，PKCβI，PKCβII，PKCγ，PKCε 和大鼠大脑 PKC 的 IC50 值为 5，24，14，27，24 和 23nM，同时能够有效抑制 MAPKAP-K1b，MSK1，S6K1 和 GSK3β (IC50，3，8，15，38nM),对 MKK3，MKK4，MKK6 和 MKK7 无作用。 靶点/IC50 PKCα (Cell-free assay) PKCβ2 (Cell-free assay) PKCβ1(Cell-free assay) PKCε (Cell-free assay) PKCγ (Cell-free assay) 5nM 14nM 24nM 24nM 27nM   体外研究 Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23nM for PK α,PKCβI,PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38nM,respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Moreover, Ro 31-8220 directly suppresses voltagedependent Na+channels. Ro 31-8220 (1μM) 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 (6mg/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.   推荐实验方法(仅供参考) 细胞实验:   A neurotoxic concentration of paraoxon (200μM) is added to the granule cell cultures for the indicated time on day in vitro (DIV) 8. The following drugs are added to the granule cell cultures prior to or after paraoxon exposure on DIV 8: Ro-81-3220 (1μM) is added 15 min prior to or 3h after the addition of paraoxon. TPA (0.1μM) is added 15 min prior to the addition of paraoxon.   动物实验:   Mice The affects of long-term Ro 31-8220 administration over 4 to 6 weeks in MLP−/− heart failure mice are investigated. All mice are assessed for ventricular performance by echocardiography at the beginning of the study and 6 weeks later. Ro 31-8220 (or vehicle) is injected subcutaneously once per day at a dosage of 6mg/kg/d.
保存条件：-20℃

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