中文名 | 阿斯利康钠盐 |
英文名 | RDEA-594 sodiuM |
别名 | 雷西纳德钠 雷西纳德钠盐 阿斯利康钠盐 雷西纳得钠盐 LESINURAD钠盐 4,4''-双(三甲基硅氧基)联苯 2-(5-溴-4-(4-环丙基萘-1-基)-4H-1,2,4-三唑-3-基硫基)乙酸钠 2-(5-溴-4-(4-环丙基萘-1-基)-4H-1,2,4-三唑-3-基硫基)乙酸乙酯钠 |
英文别名 | CS-651 RDEA-594 sodiuM LESINURAD SODIUM Lesinurad sodiuM Pentanedioicacid,5-oxo-,diethylester sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate Sodium 2-((5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3- yl)sulfanyl)acetate Acetic acid, 2-((5-bromo-4-(4-cyclopropyl-1-naphthalenyl)-4H-1,2,4-triazol-3-yl)thio)-, sodium salt |
CAS | 1151516-14-1 |
化学式 | C17H13BrN3O2S.Na |
分子量 | 426.26279 |
溶解度 | DMSO: ≥ 26 mg/mL母液保存:分装冻存,避免反复冻融;-20℃,1个月;-80℃,6个月(稀释后溶液温度低保存可能会析出,尽量现用现配)细胞实验:先用DMSO溶解:再用培养基进行稀释,稀释过程建议分段进行,避免浓度变化过快导致化合物析出。若稀释过程中出现化合物析出的情况, 可采用超声的方法使其复溶。在稀释时要确保工作液中 DMSO 的终浓度尽量在0.1%以下,最高不要超过0.5%,并设置相应浓度的DMSO对照组。动物实验:先用DMSO溶解:再用水或者生理盐水等去稀释,稀释过程建议分段进行,避免浓度变化过快导致化合物析出。若稀释过程中出现化合物析出的情况, 可采用超声的方法使其复溶。可以通过添加助溶剂来帮助溶解,比如植物油、Tween80、甘油、羧甲基纤维素钠和PEG400等。具体方式请参考文献。悬浊液可用于口服和腹腔注射,不会影响产品活性。 |
存储条件 | -20℃ |
靶点 | Km: 0.85 µM (OAT1), 2 µM (OAT3) |
上游原料 | 1-环丙基-4-异硫代氰酰基萘 4-环丙基萘-1-胺草酸盐 N-(4-环丙基-1-萘基)-2-甲酰基肼基硫代甲酰胺 叔丁基(4-环丙基萘-1-基)氨基甲酸叔丁酯 4-环丙基-1-萘胺 2-[[4-(4-环丙基萘-1-基)-4H-1,2,4-三唑-3-基]硫基]乙酸甲酯 1-环丙基萘 |
参考资料 展开查看 | 1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK547982/ PubMed PMID: 31643315. 2: Pérez-Ruiz F, Jansen T, Tausche AK, Juárez-Campo M, Gurunath RK, Richette P. Efficacy and safety of lesinurad for the treatment of hyperuricemia in gout. Drugs Context. 2019 May 29;8:212581. doi: 10.7573/dic.212581. eCollection 2019. Review. PubMed PMID: 31191704; PubMed Central PMCID: PMC6544139. 3: Dean L. Lesinurad Therapy and CYP2C9 Genotype. 2019 Feb 11. In: Pratt V, McLeod H, Rubinstein W, Dean L, Kattman B, Malheiro A, editors. Medical Genetics Summaries [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK537366/ PubMed PMID: 30742400. 4: Jansen TL, Perez-Ruiz F, Tausche AK, Richette P. International position paper on the appropriate use of uricosurics with the introduction of lesinurad. Clin Rheumatol. 2018 Dec;37(12):3159-3165. doi: 10.1007/s10067-018-4306-9. Epub 2018 Sep 22. Review. PubMed PMID: 30244431. 5: Claus LW, Saseen JJ. Patient considerations in the management of gout and role of combination treatment with lesinurad. Patient Relat Outcome Meas. 2018 Jul 18;9:231-238. doi: 10.2147/PROM.S108868. eCollection 2018. Review. PubMed PMID: 30140163; PubMed Central PMCID: PMC6054769. 6: On PC. Lesinurad (Zurampic) for Gout. Am Fam P |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.346 ml | 11.73 ml | 23.46 ml |
5 mM | 0.469 ml | 2.346 ml | 4.692 ml |
10 mM | 0.235 ml | 1.173 ml | 2.346 ml |
5 mM | 0.047 ml | 0.235 ml | 0.469 ml |
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