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.

Product information

CAS Number: 951395-08-7

Molecular Weight: 503.33

Formula: C21H24Cl2N2O8

Chemical Name: (2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol; 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid

Smiles: CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.OC(=O)C1C=C2OC(=NC2=CC=1)C1C=C(Cl)C=C(Cl)C=1

InChiKey: DQJDBUPLRMRBAB-WZTVWXICSA-N

InChi: InChI=1S/C14H7Cl2NO3.C7H17NO5/c15-9-3-8(4-10(16)6-9)13-17-11-2-1-7(14(18)19)5-12(11)20-13;1-8-2-4(10)6(12)7(13)5(11)3-9/h1-6H,(H,18,19);4-13H,2-3H2,1H3/t;4-,5+,6+,7+/m.0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 12.5 mg/mL (24.83 mM; Need ultrasonic). H2O : < 0.1 mg/mL (insoluble).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. Tafamidis (0-7.2 μM) dose-dependently inhibits WT-TTR amyloidogenesis after treatment for 72 hours at a pH of 4.4-4.5.

Products are for research use only. Not for human use.