Dihydroartemisinin-Dihydroqinghaosu-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDihydroartemisininCat. No.: HY-N0176CAS No.: 71939-50-9Synonyms: Dihydroqinghaosu; -Dihydroartemisinin; Artenimol分式: CHO分量: 284.35作靶点: Parasite; NF-B; Autophagy作通路: Anti-infection; NF-B; Autophagy储存式: Powder -20C 3 years4C 2 yea

2、rsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 41.67 mg/mL (146.54 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.5168 mL 17.5840 mL 35.1679 mL5 mM 0.7034 mL 3.5168 mL 7.0336 mL10 mM 0.3517 mL 1.7584 mL 3.5168 mL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，并请注意储备液的保存式和期限。体内实验请根据您的实

3、验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (7.31 mM); Suspended solution; Need ultrasonic and warming2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in sali

4、ne)Solubility: 2.08 mg/mL (7.31 mM); Clear solution; Need ultrasonic and warming3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (7.31 mM); Clear solution; Need warmingBIOLOGICAL ACTIVITY物活性 Dihydroartemisinin种有效的抗疟疾 (anti-malaria) 药物。IC50 &

5、Target RelA Autophagy体外研究 Dihydroartemisinin (DHA) is an antimalarial agent. Dihydroartemisinin treatment effectively up-regulates thecytosolic RelA/p65 protein level and down-regulates the nuclear RelA/p65 protein level. Dihydroartemisininblocks the nuclear translocation of RelA/p65 from the cytoso

6、l rather than suppressing RelA/p65 proteinsynthesis. Dihydroartemisinin induces autophagy in RPMI 8226 cells. Dihydroartemisinin suppresses NF-Bactivation in RPMI 8226 cells. The NF-B Dihydroartemisinin -binding activity is examined by EMSA assay.RPMI 8226 cells are exposed to various concentrations

7、 of Dihydroartemisinin (10, 20 and 40 M) for 12 h,and TNF- is introduced as a positive control for NF-B activation. Dihydroartemisinin suppresses NF-Bactivation in a dose-dependent manner in contrast with TNF- 1. Dihydroartemisinin (DHA) can enhance theanti-tumor effect of photodynamic therapy (PDT)

8、 on esophageal cancer cells, and cell viability is investigatedusing the MTT assay. Eca109 and Ec9706 cells are treated with Dihydroartemisinin (80 M), PDT (25 and 20J/cm2, respectively) or their combination. Single treatment with Dihydroartemisinin or PDT causes a 375%or 346% reduction in viability

9、 in Eca109 cells and a 337% or 346% reduction in Ec9706 cells,respectively. However, when PDT is combined with Dihydroartemisinin, the cell viability is reduced 596% or617% in the cell lines, respectively 2.体内研究 Single oral doses of Dihydroartemisinin (at 200, 300, 400 or 600 mg/kg), given once on e

10、ach 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 reducetotal-worm burdens by 73.9%-85.5% and female-worm burdens by 83.8%-95.3% 3.PROTOCOLKi

11、nase Assay 1 To determine NF-B Dihydroartemisinin-binding activity, an electrophoretic mobility shift assay (EMSA) isperformed. Nuclear extracts are prepared and incubated with 32P-end-labeled 45-mer double-strandedoligonucleotide (15 g protein with 16 fmol DNA) from the HIV long terminal repeat, 5-

12、TTGTTACAAGGGACTTTCCGCTG GGGACTTTCCAGGGAGGCGTGG-3 (boldface indicates NF-B bindingsites), for 30 min at 37 C. The Dihydroartemisinin-protein complex formed is separated from freeoligonucleotide on 6.6% native polyacrylamide gels. A double-stranded mutated oligonucleotide, 5-TTGTTACAA CTCACTTTCCGCTGCT

13、CACTTTCCAGGGAGGCGTGG-3, is used to examine bindingspecificity of NF-B to the DNA. The binding specificity is also examined by competition with the unlabeledoligonucleotide. Preimmune serum (PIS) is included as a negative control. The dried gels are visualized witha Storm 820, and radioactive bands a

14、re quantified using Imagequant software 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemECell Assay 2 Eca109 (4103 cells/well) and Ec9706 (5103 cells/well) cells are grown in 96-well plates and culturedo

15、vernight to allow for cell attachment. Eca109 and Ec9706 cells are treated with Dihydroartemisinin (80 M),PDT (25 and 20 J/cm2, respectively) or their combination. After incubation for 24h, MTT (20 L) is added toeach well and incubated for 4 h at 37C. Formazan crystals are dissolved in 150 L of DMSO

16、 for 10 min withshaking. The absorbance is measured at 490 nm on a plate reader, and the experiment is repeated threetimes 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 Mice of the Kunming strain, each weighing 20-24 g,

17、 are used. In the first experiment, design to investigatethe 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 600 mg Dihydroartemisinin/kg (in dose volumes of 25mL/kg), on days 6-8 or 34-36 post-

18、infection, respectively. An additional group of mice, infected but not giventhe drug, serve as a control.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Biochem Biophys Res Commun. 2018 Jun 27;501(3):636-642.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Hu W, et al. Dihydroartemisinin induces autophagy by suppressing NF-B activation. Cancer Lett. 2014 Feb 28;343(2):239-48.2. Li YJ, et al. Dihyd