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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETangeretinCat. No.: HY-N0133CAS No.: 481-53-8Synonyms: Tangeritin; NSC53909; NSC618905分式: CHO分量: 372.37作靶点: Notch作通路: Neuronal Signaling; Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外
2、实验 DMSO : 30 mg/mL (80.57 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.6855 mL 13.4275 mL 26.8550 mL5 mM 0.5371 mL 2.6855 mL 5.3710 mL10 mM 0.2686 mL 1.3428 mL 2.6855 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
3、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 90% corn oilSolubility: 2.5 mg/mL (6.71 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 Tangeretin (Tangeritin),酮类化合物, Notch-1的有效抑制剂,具有抗炎,保护神经等作。IC50 & Target Notch-
4、1体外研究 Tangeretin enhanced the radiosensitivity of GC cells as demonstrated by MTT and colony formation assays.Tangeretin also attenuated radiation-induced EMT, invasion and migration in GC cells, accompanied by adecrease in Notch-1, Jagged1/2, Hey-1 and Hes-1 expressions. Tangeretin triggered the up
5、regulation of miR-410, a tumor-suppressive microRNA. Furthermore, re-expression of miR-410 prevented radiation-inducedEMT and cell invasion 1.体内研究 In this study, we investigated the in vivo anti-RSV activity of tangeretin in 3-week-old male BALB/c mice. Aplaque reduction assay and fluorescence quant
6、itative polymerase chain reaction (FQ-PCR) showed thattangeretin inhibited RSV replication in the lung of mice 2.PROTOCOLCell Assay The effect of tangeretin on RAW264.7 cells was determined using a MTT assay as previously reported.(13)Briefly, RAW264.7 cells (1 104 cells/well) were seeded in a 96-we
7、ll plate for 24 h and treated with differentconcentrations of tangeretin (6.350.0 M) and dimethyl sulfoxide (DMSO) (vehicle control, 0.01 and 0.1%)for 10 or 48 h. The absorbance was measured at 570 nm using an enzyme immunoassay (EIA) reader(Thermo Scientific, Waltham, MA), and cell viability (%) wa
8、s calculated as follows: (absorbance of the testgroup absorbance of the blank control)/(absorbance of the control group absorbance of the blankcontrol) 100.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Animal administration 2 The mice were main
9、tained in an air-conditioned, pathogen-free room (temperatureAdministration of 24 2 C, with a 12 h light/dark cycle from 6:00 am to 6:00 pm) with free access to food and water. Micewere randomly divided into five groups (n = 10) as follows: normal (control), RSV-challenged, and threetreatment groups
10、 administered 25, 50, or 100 mg/kg/day tangeretin dissolved in saline. The control and RSV-challenged groups received equal volumes of saline. During the experiment, mice in the treatment groupswere intragastrically administrated tangeretin for 3 days consecutively before RSV stimulation. Mice werel
11、ightly anesthetized with diethyl ether and intranasally challenged with RSV Long strain 6.7 106 plaque-forming units (PFU) on day 4 after tangeretin treatment, while the control group was sham-infected with anequal volume of HEp-2 cell lysate, which was centrifuged under the same conditions as the v
12、iralsuspensions. The mice were weighed during the experiment and sacrificed on day 5 post-infection afteranesthetizing them with chloral hydrate (Figure 1B). The lung tissues were removed and weighed, and thelung index was calculated using the following formula: lung index = lung weight/body weight.
13、MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zhang X, et al. Tangeretin enhances radiosensitivity and inhibits the radiation-induced epithelial-mesenchymal transition of gastriccancer cells. Oncol Rep. 2015 Jul;34(1):302-10.2/3 Master of
14、 Small Molecules 您边的抑制剂师www.MedChemE2. Xu JJ, et al. Tangeretin from Citrus reticulate Inhibits Respiratory Syncytial Virus Replication and Associated Inflammation in Vivo. JAgric Food Chem. 2015 Nov 4;63(43):9520-7.3. Hagenlocher Y, et al. Citrus peel polymethoxyflavones nobiletin and tangeretin suppress LPS- and IgE-mediated activation of humanintestinal mast cells. Eur J Nutr.
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