951395-08-7

951395-08-7 structure

Name: Tafamidis meglumine
Chemical Name: tafamidis meglumine
CAS Number: 951395-08-7
Molecular Formula: C₂₁H₂₄Cl₂N₂O₈
Molecular Weight: 503.33000
Catalog: Research Areas Neurological Disease
Create Date: 2016-01-16 14:35:12
Modify Date: 2024-01-04 09:56:30
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].

Name	tafamidis meglumine
Synonyms	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

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.