货号:A225692 同义名: 他发米帝司甲葡胺 / PF-06291826
Tafamidis is a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade.
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描述 | Tafamidis functions as a potent and selective stabilizer of transthyretin (TTR), demonstrating similar potency and efficacy to the mutant homotetramers V30M-TTR, V122I-TTR, and wild type WT-TTR, with EC50 values ranging from 2.7 to 3.2 μM. Tafamidis also inhibits amyloidogenesis[1]. |
体外研究 | Tafamidis selectively binds with negative cooperativity (Kds ~2 nM and ~200 nM) to the two normally unoccupied thyroxine-binding sites of the tetramer, thereby kinetically stabilizing TTR [1]. Tafamidis (0-7.2 μM) dose-dependently inhibits WT-TTR amyloidogenesis after 72-hour treatment at a pH of 4.4-4.5 [1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.25mL 0.65mL 0.32mL |
16.23mL 3.25mL 1.62mL |
32.46mL 6.49mL 3.25mL |
CAS号 | 594839-88-0 |
分子式 | C14H7Cl2NO3 |
分子量 | 308.116 |
别名 | 他发米帝司甲葡胺 ;PF-06291826 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 35 mg/mL(113.59 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |