常山酮溴酸盐 98.1704%
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| 包装规格: | 5mg 10mg 25mg 50mg 100mg in glass bottle |
| 溶解性: | 溶于DMSO(50 mg/mL 超声) |
| 产品描述: | 基本信息 产品编号:H60004 产品名称:Halofuginone hydrobromide CAS: 64924-67-0 储存条件 粉末 -20℃ 四年 分子式: C16H18Br2ClN3O3 溶于液体 -80℃ 六个月 分子量 495.59 -20℃ 一个月 化学名: 7-Bromo-6-chloro-3-(3-((2S,3R)-3-hydroxypiperidin-2-yl)-2-oxopropyl)quinazolin-4(3H)-one hydrobromide Solubility (25°C) 体外 DMSO 50mg/mL (100.89mM; Need ultrasonic) Ethanol Water 2mg/mL (4.04mM; Need ultrasonic) 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 2.0178mL 10.0890mL 20.1780mL 5mM 0.4036mL 2.0178mL 4.0356mL 10mM 0.2018mL 1.0089mL 2.0178mL 生物活性 产品描述 Febrifugine 的一种低毒性衍生物,可从 Dichroa febrifuga 中分离出来。 靶点/IC50 prolyl-tRNA synthetase Ki: 18.3±0.5nM 体外研究 Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase. The IC50s of Halofuginone (1, 10, 100, 1000, 10000nM; 48 hours) are 114.6 and 58.9nM in KYSE70 and A549 cells, respectively. The IC50s of Halofuginone (1, 10, 100, 1000nM; 24 hours) for NRF2 protein are 22.3 and 37.2nM in KYSE70 and A549 cells,respectively. The IC50 of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively. Halofuginone increases voltage-gated K+ (Kv) currents in pulmonary artery smooth muscle cells (PASMC) and K+ currents through KCNA5 channels in HEK cells transfected with KCNA5 gene. Halofuginone (0.03-1μM) inhibits receptor-operated Ca2+ entry (ROCE) in HEK cells transfected with calcium-sensing receptor gene and attenuated store-operated (SOCE) Ca2+ entry in PASMC. Cell Viability Assay Cell Line: KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring theKEAP1 gene mutation Concentration: 1, 10, 100, 1000, 10000nM Incubation Time: 48 hours Result: The IC50s were 114.6 and 58.9nM in KYSE70 and A549 cells, respectively. Western Blot Analysis Cell Line: KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring theKEAP1 gene mutation Concentration: 1, 10, 100, 1000nM Incubation Time: 24 hours Result: The IC50s for NRF2 protein were 22.3 and 37.2nM in KYSE70 and A549 cells, respectively. |
| 保存条件: | -20℃ |
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