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Tafamidis meglumine

Names

[ CAS No. ]:
951395-08-7

[ Name ]:
Tafamidis meglumine

[Synonym ]:
Vyndaqel
UNII-ZU7CF08A1A
Tafamidis meglumine
2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid,(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol
ZU7CF08A1A
Fx-1006A

Biological Activity

[Description]:

Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[Target]

EC50: 2.7-3.2 μM (TTR)[1]


[In Vitro]

Tafamidis binds selectively and with negative cooperativity (Kds ∼2 nM and ∼200 nM) to the two normally unoccupied thyroxine-binding sites of the tetramer, and kinetically stabilizes TTR[1]. Tafamidis (0-7.2 μM) dose-dependently inhibits WT-TTR amyloidogenesis after treatment for 72 hours at a pH of 4.4-4.5[1].

[References]

[1]. Bulawa CE, et al. 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.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H24Cl2N2O8

[ Molecular Weight ]:
503.33000

[ Exact Mass ]:
502.09100

[ PSA ]:
176.51000

[ LogP ]:
1.53240

[ Storage condition ]:
2-8℃

Related Compounds