MBP146-78 ≥98%
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| 包装规格: | 1mg 5mg 10mg 25mg 50mg in glass bottle |
| 溶解性: | 溶于DMSO(7.69 mg/mL 超声) |
| 产品描述: | 基本信息 产品编号:M10672 产品名称:MBP146-78 CAS: 188343-77-3 储存条件 粉末 -20℃ 四年 分子式: C21H22FN3 溶于液体 -80℃ 两年 分子量 335.42 -20℃ 一个月 化学名: 4-(2-(4-fluorophenyl)-5-(1-methylpiperidin-4-yl)-1H-pyrrol-3-yl)pyridine Solubility (25°C) 体外 DMSO 12mg/mL (35.77mM) Ethanol 12mg/mL (35.77mM) 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 2.9813mL 14.9067mL 29.8134mL 5mM 0.5963mL 2.9813mL 5.9627mL 10mM 0.2981mL 1.4907mL 2.9813mL 生物活性 产品描述 有效的选择性的cGMP依赖的蛋白激酶抑制剂。 靶点/IC50 PKG() 体外研究 MBP146-78 displays a dose-dependent inhibition of T. gondii tachyzoites replicating inside HFFs, with an IC50 of 210nM. The suppression of lytic parasite growth by MBP146-78 is reversible. Replacement of the medium with medium lacking MBP146-78, after treatment for up to 7 days at 2μM, results in complete lysis of HFF cell monolayers. MBP146-78 is neither toxic nor inhibitory to proliferating or confluent monolayers of HFFs at concentrations of up to 10μM. 体内研究 In infected mice that are treated with MBP146-78 at 50mg/kg twice daily, parasites are undetectable throughout the 10-day treatment period in each of the tissues examined. However, samples from brain, spleen, and lung taken from infected treated mice reveal the presence of parasites after cessation of administration of MBP146-78, indicating that a transient asymptomatic parasite recrudescence occurs in all survivors. The ability of mice to control Toxoplasma infection after MBP146-78 treatment has been terminated suggests that the mouse immune system plays a synergistic role with chemotherapy in controlling the infection. 推荐实验方法(仅供参考) 细胞实验: Cell Assay To assess the toxicity of MBP146-78 to HFFs, cells are plated in 96-well plates at 1000/well and allowed to adhere overnight prior to addition of compound. Cultures are incubated for 5 days at 37°C in the presence of 5% CO2. Viability is assessed using the Cell-Titer 96 Aqueous One solution cell-proliferating assay. 动物实验: Animal Administration Mice: MBP146-78 is dissolved in water. MBP146-78 is administered in 100μL doses by intraperitoneal injections starting 24h after parasite inoculation. Mice are monitored twice daily for clinical evidence of toxoplasmosis and mortality throughout the experimental period. |
| 保存条件: | -20℃ |
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