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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDocosahexaenoic AcidCat. No.: HY-B2167CAS No.: 6217-54-5Synonyms: DHA; Cervonic Acid分式: CHO分量: 328.49作靶點(diǎn): Endogenous Metabolite作通路: Metabolic Enzyme/Protease儲(chǔ)存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 mo
2、nth (stored undernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn) Ethanol : 50 mg/mL (152.21 mM; Need ultrasonic)DMSO : 5.2 mg/mL (15.83 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 0.52 mg/mL (1.58 mM); Clear solution2. 請(qǐng)依序添加每種溶劑: 10% DMSO 90% corn oilSolubility: 0.52 mg/mL (1.58 mM); Clear solution1/3
3、 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑: 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 5 mg/mL (15.22 mM); Clear solution4. 請(qǐng)依序添加每種溶劑: 10% EtOH 90% (20% SBE-CD in saline)Solubility: 5 mg/mL (15.22 mM); Suspended solution; Need ultrasonic5. 請(qǐng)依序添加每種溶劑: 10% EtOH 90% corn oilS
4、olubility: 5 mg/mL (15.22 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Docosahexaenoic Acid (DHA)豐富地存在于腦和視膜中的-3脂肪酸,可以直接從魚(yú)油和母乳中獲得。IC50 & Target Human Endogenous Metabolite體外研究 Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants.DHA is also required f
5、or maintenance of normal brain function in adults. The inclusion of plentiful DHA in thediet improves learning ability and memory 1. DHA is an essential requirement in every step of braindevelopment like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple doublebonds
6、and unique structure allow DHA to impart special membrane characteristics for effective cell signaling.Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder,schizophrenia etc. are causally related to decreased level of DHA 2. DHA is a potent RXR
7、 ligand inducingrobust RXR activation already at low micro molar concentrations. The EC50 for RXR activation by DHA isabout 5-10 M fatty acid 3.體內(nèi)研究 Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memoryerrors, without affecting the number of working m
8、emory errors, and significantly increases thedocosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampusand the cerebral cortex 4. DHA treatment exerts neuroprotective actions on an experimental mouse modelof PD. There is a decrease tendency in brain lipi
9、d oxidation of MPTP mice but it does not significantly 5.PROTOCOLAnimal Rats: Wistar rats are fed a fish oil-deficient diet through three generations. The young (five-week-old) maleAdministration 45 rats of the third generation are randomLy divided into two groups. Over 10 weeks, one group is perora
10、llyadministered docosahexaenoic acid dissolved in 5% gum Arabic solution at 300 mg/kg/day; the other groupreceives a similar volume of vehicle alone. Five weeks after starting the administration, the rats are tested forlearning ability related to two types of memory, reference memory and working mem
11、ory, with the partially(four of eight) baited eight-arm radial maze 4.Mice: An experimental model of Parkinsons disease is created by four intraperitoneal injections of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) (420 mg/kg, at 12 h intervals). Docosahexaenoic acid is givendaily by gavage fo
12、r 4 weeks (36 mg/kg/day). The motor activity of the mice is evaluated via the pole test. Theactivity of antioxidant enzymes in the brain are determined by spectrophotometric assays and theconcentration of thiobarbituric acid-reactive substances (TBARS) are measured as an index of oxidative2/3 Master
13、 of Small Molecules 您邊的抑制劑師www.MedChemEdamage 5.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Horrocks LA, et al. Health benefits of docosahexaenoic acid (DHA). Pharmacol Res. 1999 Sep;40(3):211-25.2. Gharami K, et al. Essential role of d
14、ocosahexaenoic acid towards development of a smarter brain. Neurochem Int. 2015 Oct;89:51-62.3. Lengqvist J, et al. Polyunsaturated fatty acids including docosahexaenoic and arachidonic acid bind to the retinoid Xreceptor alphaligand-binding domain. Mol Cell Proteomics. 2004 Jul;3(7):692-703.4. Gamoh S, et al. Chronic administration of docosahexaenoic acid improves reference memory-related learning ability in young rats.Neuroscience. 1999;93(1):237-41.5. Ozsoy O, et al. The influence and the mechanism of docosahexaenoic acid on a mouse model of Parkinsons disease. Neurochem Int
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