|(2R,3R,4R,5S)-6-(甲氨基)己烷-1,2,3,4,5-五醇 2-(3,5-二氯苯基)苯并[d]恶唑-6-羧酸盐|CsnPharm

CAS No.: 951395-08-7

Tafamidis meglumine/他发米帝司甲葡胺 Catalog No. CSN24476

Synonyms: Fx-1006A;PF-06291826;他发米帝司甲葡胺

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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实验方案

技术信息

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 .
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9868 mL
- 9.9338 mL
- 19.8677 mL
- 5 mM
- 0.3974 mL
- 1.9868 mL
- 3.9735 mL
- 10 mM
- 0.1987 mL
- 0.9934 mL
- 1.9868 mL

技术信息

CAS号

951395-08-7

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H24Cl2N2O8

运输

蓝冰

分子量

503.33

别名

Fx-1006A;PF-06291826;他发米帝司甲葡胺

溶解度

DMSO	11.67 mg/mL (23.2 mM)
Water	insoluble

动物实验配方

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Tafamidis meglumine/他发米帝司甲葡胺 Catalog No. CSN24476

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