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他发米帝司甲葡胺 /Tafamidis meglumine {[allProObj[0].p_purity_real_show]}

货号:A1167264 同义名: Fx-1006A

Tafamidis meglumine选择性地结合并通过负协同作用(K(d)s ~2 nM 和 ~200 nM)结合四聚体的两个正常未被占据的甲状腺素结合位点,并稳定 TTR(甲状腺素转运蛋白)。

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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+
Tafamidis meglumine 化学结构 CAS号:951395-08-7
Tafamidis meglumine 化学结构
CAS号:951395-08-7
Tafamidis meglumine 3D分子结构
CAS号:951395-08-7
Tafamidis meglumine 化学结构 CAS号:951395-08-7
Tafamidis meglumine 3D分子结构 CAS号:951395-08-7
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Tafamidis meglumine 纯度/质量文件 产品仅供科研

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Tafamidis meglumine 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 .

Tafamidis meglumine 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.

Tafamidis meglumine 实验方案

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

Tafamidis meglumine 技术信息

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

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Room Temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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