Dihydroartemisinin-Dihydroqinghaosu-DataSheet-生命科學試劑-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作靶點: Parasite; NF-B; Autophagy作通路: Anti-infection; NF-B; Autophagy儲存式: Powder -20C 3 years4C 2 yea

2、rsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 41.67 mg/mL (146.54 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實

3、驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (7.31 mM); Suspended solution; Need ultrasonic and warming2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in sali

4、ne)Solubility: 2.08 mg/mL (7.31 mM); Clear solution; Need ultrasonic and warming3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (7.31 mM); Clear solution; Need warmingBIOLOGICAL ACTIVITY物活性 Dihydroartemisinin種有效的抗瘧疾 (anti-malaria) 藥物。IC50 &

5、Target RelA Autophagy體外研究 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.體內(nèi)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 您邊的抑制劑師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.戶使本產(chǎn)品發(fā)表的科研獻 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