Tafamidis binds selectively and with negative cooperativity (K(d)s ~2 nM and ~200 nM) to the two normally unoccupied thyroxine-binding sites of the tetramer, and kinetically stabilizes TTR.
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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免费溶解
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 . |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.99mL 0.40mL 0.20mL |
9.93mL 1.99mL 0.99mL |
19.87mL 3.97mL 1.99mL |
CAS号 | 951395-08-7 |
分子式 | C21H24Cl2N2O8 |
分子量 | 503.33 |
别名 | Fx-1006A |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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 |
动物实验配方 |