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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECiticolineCat. No.: HY-B0739CAS No.: 987-78-0Synonyms: cytidine diphosphate-choline; CDP-Choline; cytidine 5-diphosphocholine分式: CHNOP分量: 488.32作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C
2、 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 103.33 mg/mL (211.60 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.0478 mL 10.2392 mL 20.4784 mL5 mM 0.4096 mL 2.0478 mL 4.0957 mL10 mM 0.2048 mL 1.0239 mL 2.0478 mL請(qǐng)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(chǔ)備液,并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVI
3、TY物活性 Citicoline種合成細(xì)胞膜組分磷脂酰膽堿的中間體。發(fā)揮神經(jīng)保護(hù)作。體外研究To determine the potential neuroprotective activity of Citicoline and Homotaurine, treated retinal cells aretreated with increasing concentrations of Citicoline or Homotaurine for 24 hours. 1M, 10M and 100M of1/3 Master of Small Molecules 您邊的抑制劑師www.MedC
4、hemECiticoline or Homotaurine are used to investigate whether may contribute to a reduced cell viability in retinalcells. Retinal cells are well preserved in Citicoline- or Homotaurine-treated cultures, with no evidence oftoxicity or significant loss of viability after treatments. 100M of Citicoline
5、 is not harmful to retinal neuroglialcells in vitro and 100M of Homotaurine is an effective concentration to enhance neuroprotection in a modelof experimental glaucoma. Therefore, this concentration of Citicoline and Homotaurine is used for allsubsequent experiments. To evaluate whether cotreatment
6、with Citicoline and Homotaurine is able to inducea synergistic neuroprotective effect against glutamate excitotoxicity, retinal cell cultures are exposed toCiticoline 100M, Homotaurine 100M, and Citicoline+Homotaurine 100M, 24 hours before glutamatetreatment. In the presence of 100M Citicoline, a si
7、gnificant increase in cell viability is observed 1.體內(nèi)研究 Administration of Citicoline in a dose of 1000 mg/kg produces more pronounced increase in the threshold ofclonic seizures and tonic phase of seizures with lethal outcome (by 18.54 and 50.08% respectively, incomparison with the control). The ant
8、iconvulsant effect is most pronounced after injection of Citicoline in adose of 1000 mg/kg 2.PROTOCOLCell Assay 1 The assay used to assess cell viability in retinal cells was the MTT reduction assay. To evaluate the effect ofCiticoline and Homotaurine on cell survival, the cells are subdivided into
9、three groups and treated for 24hours with 1M, 10M, and 100M of Citicoline and with 1M, 10M and 100M of Homotaurine. Toevaluate the neuroprotective effects of Citicoline and Homotaurine, cells are treated with Citicoline 100M,Homotaurine 100M, or Citicoline+Homotaurine 100M, 24 hours before glutamate
10、 treatment and 30minbefore high glucose (HG) treatment. MTT is added to wells at a final concentration of 0.5mg/mL for 1 hour at37C. After this time, the medium is removed and reduced MTT (blue formazan product) is solubilized byadding 100L DMSO to each well. After agitation of plates for 15min, the
11、 optical density of the solubilizedformazan product in each well is measured using an automatic microplate reader with a 570nm testwavelength and a 690nm reference wavelength 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration
12、1 Experiments are performed on male C57Bl/6 mice (n=69) weighing 23-27 g. The study is performed in twoseries. In series I, the dose-dependent effect of Citicoline on the seizure threshold in mice is evaluated. Themeasurements are performed 1 h after Citicoline administration. Citicoline in doses of
13、 500 and 1000 mg/kg(0.04 mL per 20 g body weight) is injected intraperitoneally. The control animals receive an equivalentvolume of physiological saline under similar conditions. In series II, the duration of Citicoline effect isestimated in 3 and 6 h after single intraperitoneal injection of Citico
14、line.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Davinelli S, et al. Cytoprotective Effects of Citicoline and Homotaurine against Glutamate and High Glucose Neurotoxicity in PrimaryCultured Retinal Cells. Oxid Med Cell Longev. 2017;2017:2825703.2. Karpova MN, et al. Increase of the seizure threshold in C57BL/6 mice after citicoline administration. Bull Exp Biol Med. 20152/3 Master of Small Molecules 您邊的抑制劑師www.MedChem
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