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Tafamidis meglumine

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Chemical Structure| 951395-08-7 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

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:
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

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

[1]Bulawa CE, Connelly S, Devit M, Wang L, Weigel C, Fleming JA, Packman J, Powers ET, Wiseman RL, Foss TR, Wilson IA, Kelly JW, Labaudinière R. 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. doi: 10.1073/pnas.1121005109. Epub 2012 May 29. PMID: 22645360; PMCID: PMC3386102.