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Tafamidis

Tafamidis (Fx-1006A) 是选择性的transthyretin (TTR)稳定剂，对野生型 WT-TTR 、突变型同源四聚体 V30M-TTR、V122I-TTR 的活性相当，它们的EC50值为2.7-3.2 μM。它对淀粉样蛋白的生成具有抑制作用。

CAS号

594839-88-0

分子式

C14H7Cl2NO3

主要靶点

Others

仅限科研使用

Cat No : CM06818

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Synonyms

氯苯唑酸|Fx-1006A|他发米帝司甲葡胺

验证数据展示

  • CAS No.: 594839-88-0

    Tafamidis
    CAS#: 594839-88-0

产品信息

Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs. It binds to TTR with negative cooperativity (Kd1: 3 nM; Kd2: 278 nM) to stabilize the TTR dimer-dimer interface and inhibit tetrameric dissociation. Tafamidis stabilizes wild-type and clinically significant V30M and V122I mutant TTR amyloidogenic homotetramers (EC50s: 2.7-3.2 μM) under fibril-promoting, denaturing, and physiological conditions in vitro. It stabilizes TTR heterotetramers containing wild-type and mutant subunits ex vivo in human plasma derived from patients carrying V30M or V1221 mutations when used at a concentration of 7.2 μM. Formulations containing tafamidis have been used for the treatment of familial amyloid polyneuropathy.

CAS号 594839-88-0
分子式 C14H7Cl2NO3
主要靶点 Others
主要通路 其他
分子量 308.12
纯度 99.48%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 氯苯唑酸|Fx-1006A|他发米帝司甲葡胺

靶点活性

V30M and V122I mutant TTR amyloidogenic homotetramers:2.7-3.2 μM(ec50)

溶解度

Ethanol:2 mg/mL,DMSO:10 mg/mL

参考文献

1.Bulawa, C.E., et al., Tafamidis, a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade. Proc Natl Acad Sci U S A, 2012. 109(24): p. 9629-34.
2.Scott L J. Tafamidis: A Review of Its Use in Familial Amyloid Polyneuropathy[J]. Drugs, 2014, 74(12):1371.

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