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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDeferasirox Fe3+ chelateCat. No.: HY-16564CAS No.: 554435-83-5分式: CHFeNO分量: 426.18作靶點: Others作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 50 mg/mL (117.32 mM; Need ultrasonic)

2、Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3464 mL 11.7321 mL 23.4643 mL5 mM 0.4693 mL 2.3464 mL 4.6929 mL10 mM 0.2346 mL 1.1732 mL 2.3464 mL請根據產品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液,并請注意儲備液的保存式和期限。體內實驗 請根據您的實驗動物和給藥式選擇適當的溶解案,配制前請先配制澄清的儲備液,再依次添加助溶劑(為保證實驗結果的可靠性,體內實驗的作液,建議您現現配,當天使;澄清的儲備液可以根據儲存條件,適當保存;以下溶劑

3、前的百分 指該溶劑在您配制終溶液中的體積占):1. 請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.87 mM); Clear solution2. 請依序添加每種溶劑: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.87 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Defera

4、sirox Fe3+ chelate服的鐵螯合劑。體外研究 Deferasirox is the first oral medication approved in the USA for this purpose. The half-life of deferasirox isbetween 8 and 16 hours allowing once a day dosing. Two molecules of deferasirox are capable of binding to1 atom of iron which are subsequently eliminated by fec

5、al excretion. Its low molecular weight and highlipophilicity allows the drug to be taken orally unlike desferoxamine which has to be administered by IV route(intravenous infusion). Together with deferiprone, deferasirox seems to be capable of removing iron fromcells (cardiac myocytes and hepatocytes

6、) as well as removing iron from the blood.REFERENCES1. Yang LP, Keam SJ, Keating GM. Deferasirox : a review of its use in the management of transfusional chronic iron overload. Drugs.2007;67(15):2211-30.2. Kontoghiorghes GJ. Introduction of higher doses of deferasirox: better efficacy but not effect

7、ive iron removal from the heart andincreased risks of serious toxicities. Expert Opin Drug Saf. 2010 Jul;9(4):633-41.3. Galanello R, Campus S, Origa R. Deferasirox: pharmacokinetics and clinical experience. Expert Opin Drug Metab Toxicol. 2012Jan;8(1):123-34.4. Donnelly JP, Lahav M. Deferasirox as a

8、djunctive therapy for mucormycosis. J Antimicrob Chemother. 2012 Mar;67(3):519-20.5. Lui GY, Obeidy P, Ford SJ et al. The Iron Chelator, Deferasirox, as a Novel Strategy for Cancer Treatment: Oral Activity Against HumanLung Tumor Xenografts and Molecular Mechanism of Action. Mol Pharmacol. 2012 Oct 16. Epub ahead of printMcePdfHeightCaution: Product has not been fully validated for medical application

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