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. |