Nicaraven-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENicaravenCat. No.: HY-100592CAS No.: 79455-30-4分式: CHNO分量: 284.31作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) 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制備儲(chǔ)備液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。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您

3、現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (9.67 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (9.67 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.Med

4、ChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (9.67 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Nicaraven種新穎的化學(xué)合成的羥 由基清除劑。體外研究 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.體內(nèi)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 您邊的抑制劑師www.MedChemEMcePdfHeightCa