Tafamidis meglumine (Synonyms: 他发米帝司甲葡胺; Fx-1006A)
目录号: PL09220 纯度: ≥99%
CAS No. :951395-08-7
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中文名称
Tafamidis meglumine
中文别名
2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid,(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol;他发米帝司甲葡胺
英文名称
Tafamidis meglumine
英文别名
Tafamidis meglumine;Fx1006A;Fx 1006A;ZU7CF08A1A;Tafamidis meglumine [USAN:INN];Vyndaqel (TN);Tafamidis meglumine (JAN/USAN);SB16821;D-Glucitol, 1-deoxy-1-(methylamino)-, 2-(3,5-dichlorophenyl)-6-benzoxazolecarboxylate;D09674;2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid--1-deoxy-1-(methylamino)-D-glucitol (1/1);2-(3,5-Dichlorophenyl)-1,3-benzoxazole-6-carboxyli;Fx-1006A;Vyndaqel
Cas No.
951395-08-7
分子式
C21H24Cl2N2O8
分子量
503.33
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Tafamidis meglumine (Fx-1006A) 是一种有效、选择性的 transthyretin (TTR) 稳定剂,对野生型 WT-TTR 和突变型同源四聚体 V30M-TTR,V122I-TTR 的活性相当,EC50 值为 2.7-3.2 μM。Tafamidis meglumine 抑制淀粉样蛋白的生成。
生物活性
Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC 50 s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis.
性状
Solid
IC50 & Target[1][2]
EC50: 2.7-3.2 μM (TTR)
体外研究(In Vitro)
Tafamidis binds selectively and with negative cooperativity (Kds ~2 nM and ~200 nM) to the two normally unoccupied thyroxine-binding sites of the tetramer, and kinetically stabilizes TTR.
Tafamidis (0-7.2 μM) dose-dependently inhibits WT-TTR amyloidogenesis after treatment for 72 hours at a pH of 4.4-4.5. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Bulawa CE, et al. Tafamidis, a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade. Proc Natl Acad Sci U S A. 2012 Jun 12;109(24):9629-34.
溶解度数据
In Vitro: DMSO : 12.5 mg/mL (24.83 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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