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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENicaravenCat. No.: HY-100592CAS No.: 79455-30-4分式: CHNO分量: 284.31作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (351.73 mM)H2O : 50 mg/mL (175.86 mM)* means
2、 soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.5173 mL 17.5864 mL 35.1729 mL5 mM 0.7035 mL 3.5173 mL 7.0346 mL10 mM 0.3517 mL 1.7586 mL 3.5173 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靠性,体内实验的作液,建议您
3、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: 2.75 mg/mL (9.67 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (9.67 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.Med
4、ChemE3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (9.67 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Nicaraven种新颖的化学合成的羟 由基清除剂。体外研究 The maximum aggregation rate induced by adenosine diphosphate (ADP) is significantly inhibited bynicaraven at concentration ranges of 350 M or higher in the h
5、ealthy volunteer platelets. The maximumaggregation rate induced by collagen is significantly inhibited by 1.75 mM of nicaraven 1.体内研究 Nicaraven inhibits lipid peroxidation in the liver, improves hepatic and systemic hemodynamics and energymetabolism, and suppresses liver enzyme release, endothelin-1
6、 elevation in hepatic venous blood, histologicdamage, and neutrophil infiltration into the liver 1. Nicaraven increases the number of c-kit(+)stem/progenitor cells in bone marrow and peripheral blood, with a recovery rate around 60-90% of age-matched non-irradiated healthy mice. The potency of colon
7、y forming from hematopoietic stem/progenitorcells as indicator of function is completely protected with nicaraven treatment 2. Administration of nicaravensignificantly increases the number, improves the colony-forming capacity, and decreases the DNA damage ofhematopoietic stem/progenitor cells. The
8、urinary levels of 8-oxo-2-deoxyguanosine, a marker of DNAoxidation, are significantly lower in mice that are given nicaraven compared with those that receive aplacebo. The administration of nicaraven significantly decreases the levels of the inflammatory cytokines IL-6and TNF- in the plasma of mice
9、3.PROTOCOLAnimal Mice: To investigate the protective effect and related mechanisms of nicaraven on radiation-induced injury inAdministration 3 hematopoietic stem/progenitor cells, 12 mice are exposed to 1 Gy -rays daily for 5 days in succession (atotal of 5 Gy) and are then given intraperitoneal inj
10、ections of nicaraven (100 mg/kg/day, Nicaraven group;n=6) or saline only (Placebo group; n=6), respectively, soon after each exposure. The mice are sacrificed 2days after the last exposure, and samples of urine, blood, and bone marrow cells are collected and used forthe following experiments 3.MCE h
11、as not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Komiya T, et al. A novel free radical scavenger, nicaraven, inhibits human platelet aggregation in vitro. Clin Neuropharmacol. 1999 Jan-Feb;22(1):11-4.2. Yokota R, et al. A novel hydroxyl radical s
12、cavenger, nicaraven, protects the liver from warm ischemia and reperfusion injury. Surgery.2000 Jun;127(6):661-9.3. Ali H, et al. The potential benefits of nicaraven to protect against radiation-induced injury in hematopoietic stem/progenitor cells withrelative low dose exposures.4. Nicaraven attenuates radiation-induced injury in hematopoietic stem/progenitor cells in mice. PLoS One. 2013;8(3):e60023.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdfHeightCa
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