Tafamidis meglumine

Cas No.:	951395-08-7
Chemical Name:	2-(3,5-Dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid
Synonyms:	Tafamidis,cas 594839-88-0,PF-06291826,PF06291826
SMILES:	OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CNC.O=C(C1=CC=C2N=C(C3=CC(Cl)=CC(Cl)=C3)OC2=C1)O
Formula:	C₂₁H₂₄Cl₂N₂O₈
M.Wt:	503.33
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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].
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.

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