产品说明书
Tafamidis meglumine
 |
同义名 : | Fx-1006A |
| CAS号 : | 951395-08-7 | |
| 货号 : | A1167264 | |
| 分子式 : | C21H24Cl2N2O8 | |
| 纯度 : | 98% | |
| 分子量 : | 503.33 | |
| MDL号 : | MFCD28502032 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 12 mg/mL(23.84 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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The transthyretin amyloidoses (ATTR) are caused by aggregation of transthyretin (TTR), a natively tetrameric protein involved in the transport of thyroxine and the vitamin A–retinol-binding protein complex[1]. Tafamidis meglumine is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutant homotetramers V30M-TTR, V122I-TTR and wild-type TTR (WT-TTR), with EC50s of 2.7-3.2 μM[1]. It has recently completed Phase II/III trials for the treatment of Transthyretin Type Familial Amyloid Polyneuropathy (TTR-FAP) and demonstrated a slowing of disease progression in patients heterozygous for the V30M TTR mutation. Patient-derived amyloidogenic variants of TTR, including kinetically and thermodynamically less stable mutants, are also stabilized by tafamidis binding[1]. | ||
| 作用机制 | Tafamidis binds to the weaker dimer–dimer interface of transthyretin . | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.99mL 0.40mL 0.20mL |
9.93mL 1.99mL 0.99mL |
19.87mL 3.97mL 1.99mL |
| 参考文献 |
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