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包装规格：20mg in glass bottle
产品描述：基本信息 产品编号： D10168 产品名称： Dihydroartemisinin CAS: 71939-50-9   储存条件 粉末 室温 四年     分子式： C15H24O5 溶于液体 -80℃ 两年 分子量 284.35 -20℃ 一个月 化学名：  (3r,5as,6r,8as,9r,10s,12r,12ar)-decahydro-3,6,9-trimethyl-3,12-epoxy-12h-pyrano[4,3-j][1,2]benzodioxepin-10-ol Solubility (25°C)：   体外:   DMSO 28.25mg/mL (99.34mM) Ethanol 7mg/mL (24.61mM) Water Insoluble 体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: 2.08mg/mL (7.31mM); Suspended solution; Need ultrasonic and warming 此⽅案可获得 2.08mg/mL (7.31mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。 以 1mL ⼯作液为例，取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加⼊ 50μL Tween-80，混合均匀；然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility: 2.08mg/mL (7.31mM); Clear solution; Need ultrasonic and warming 此⽅案可获得 2.08mg/mL (7.31mM) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀。 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility: 2.08mg/mL (7.31mM); Clear solution; Need warming 此⽅案可获得 2.08mg/mL (7.31mM) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例，取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中，混合均匀。 4.请依序添加每种溶剂：10% EtOH→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 1mg/mL (3.52mM); Clear solution 此⽅案可获得 ≥ 1mg/mL (3.52mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 10.0mg/mL 的澄清 EtOH 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加⼊ 50 μ L Tween-80，混合均匀；然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 5.请依序添加每种溶剂：10% EtOH→90% (20% SBE-β-CD in saline) Solubility: ≥ 1mg/mL (3.52mM); Clear solution 此⽅案可获得 ≥ 1mg/mL (3.52mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 10.0mg/mL 的澄清 EtOH 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀 。 6.请依序添加每种溶剂：10% EtOH→90% corn oil Solubility: ≥ 1mg/mL (3.52mM); Clear solution 此⽅案可获得 ≥ 1mg/mL (3.52mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例，取 100μL 10.0mg/mL 的澄清 EtOH 储备液加到 900μL ⽟⽶油中，混合均匀。 ＜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 3.5168mL 17.5840mL 35.1679mL 5mM 0.7034mL 3.5168mL 7.0336mL 10mM 0.3517mL 1.7584mL 3.5168mL 50mM 0.0703mL 0.3517mL 0.7034mL   生物活性 产品描述 Dihydroartemisinin是⼀种有效的抗疟疾 (anti-malaria) 药物。 靶点 NF-κB  体外研究 Dihydroartemisinin (DHA) is an antimalarial agent. Dihydroartemisinin treatment effectively up-regulates the cytosolic RelA/p65 protein level and down-regulates the nuclear RelA/p65 protein level. Dihydroartemisinin blocks the nuclear translocation of RelA/p65 from the cytosol rather than suppressing RelA/p65 protein synthesis. Dihydroartemisinin induces autophagy in RPMI 8226 cells. Dihydroartemisinin suppresses NF-κB activation in RPMI 8226 cells. The NF-κB Dihydroartemisinin -binding activity is examined by EMSA assay. RPMI 8226 cells are exposed to various concentrations of Dihydroartemisinin (10, 20 and 40μM) for 12 h, and TNF-α is introduced as a positive control for NF-κB activation. Dihydroartemisinin suppresses NF-κB activation in a dose-dependent manner in contrast with TNF-α. Dihydroartemisinin (DHA) can enhance the anti-tumor effect of photodynamic therapy (PDT) on esophageal cancer cells, and cell viability is investigated using the MTT assay. Eca109 and Ec9706 cells are treated with Dihydroartemisinin (80μM), PDT (25 and 20 J/cm 2 , respectively) or their combination. Single treatment with Dihydroartemisinin or PDT causes a 37±5% or 34±6% reduction in viability in Eca109 cells and a 33±7% or 34±6% reduction in Ec9706 cells, respectively. However, when PDT is combined with Dihydroartemisinin, the cell viability is reduced 59±6% or 61±7% in the cell lines, respectively 体内研究 Single oral doses of Dihydroartemisinin (at 200, 300, 400 or 600mg/kg), given once on each of day 6-8 post-infection, reduce total-worm burdens by 69.2%-90.6% and female-worm burdens by 62.2%-92.2%, depending on dosage in the first experiment. Similar treatments given on day 34-36 post-infection reduce total-worm burdens by 73.9%-85.5% and femaleworm burdens by 83.8%-95.3%.   推荐实验方法(仅供参考) Kinase Assay To determine NF-κB Dihydroartemisinin-binding activity, an electrophoretic mobility shift assay (EMSA) is performed. Nuclear extracts are prepared and incubated with 32P-end-labeled 45-mer double-stranded oligonucleotide (15μg protein with 16 fmol DNA) from the HIV long terminal repeat, 5′-TTGTTACAAGGGACTTTCCGCTG GGGACTTTCCAGGGAGGCGTGG-3′ (boldface indicates NF-κB binding sites), for 30 min at 37 °C. The Dihydroartemisinin-protein complex formed is separated from free oligonucleotide on 6.6% native polyacrylamide gels. A double-stranded mutated oligonucleotide, 5′-TTGTTACAA CTCACTTTCCGCTGCTCACTTTCCAGGGAGGCGTGG-3′, is used to examine binding specificity of NF-κB to the DNA. The binding specificity is also examined by competition with the unlabeled oligonucleotide. Preimmune serum (PIS) is included as a negative control. The dried gels are visualized with a Storm 820, and radioactive bands are quantified using Imagequant software     Cell Assay Eca109 (4×103 cells/well) and Ec9706 (5×103 cells/well) cells are grown in 96-well plates and cultured overnight to allow for cell attachment. Eca109 and Ec9706 cells are treated with Dihydroartemisinin (80μM), PDT (25 and 20 J/cm2 , respectively) or their combination. After incubation for 24h, MTT (20μL) is added to each well and incubated for 4 h at 37°C. Formazan crystals are dissolved in 150μL of DMSO for 10 min with shaking. The absorbance is measured at 490 nm on a plate reader, and the experiment is repeated three times     Animal Administration Mice Mice of the Kunming strain, each weighing 20-24 g, are used. In the first experiment, design to investigate the effect of multiple doses of Dihydroartemisinin on the schistosomula and adult worms of S. japonicum, mice are given three daily doses, of 200, 300, 400 or 600mg Dihydroartemisinin/kg (in dose volumes of 25mL/kg), on days 6-8 or 34-36 post-infection, respectively. An additional group of mice, infected but not given the drug, serve as a control.
保存条件：室温

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