Tafamidis | B3035

Tafamidis is a potent kinetic stabilizer of transthyretin (TTR). Tafamidis binds selectively and with negative cooperativity (Kd values ∼2 nM and ∼200 nM) to the two normally unoccupied thyroxine-binding sites of the tetramer and kinetically stabilizes TTR. It prevents tetramer dissociation, the rate-limiting step in TTR misfolding and amyloidogenesis. Tafamadis also binds and stabilizes patient-derived amyloidogenic variants of TTR, including kinetically and thermodynamically less stable mutants. It is approved for the treatment of cardiomyopathy caused by transthyretin mediated amyloidosis in adults.

Tafamidis is a potent kinetic stabilizer of transthyretin (TTR). Tafamidis binds selectively and with negative cooperativity (Kd values ∼2 nM and ∼200 nM) to the two normally unoccupied thyroxine-binding sites of the tetramer and kinetically stabilizes TTR. It prevents tetramer dissociation, the rate-limiting step in TTR misfolding and amyloidogenesis. Tafamadis also binds and stabilizes patient-derived amyloidogenic variants of TTR, including kinetically and thermodynamically less stable mutants. It is approved for the treatment of cardiomyopathy caused by transthyretin mediated amyloidosis in adults.

B3035 | Tafamidis DataSheet

Alternate Name/Synonyms: FX-1006; 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid; 2-(3,5-Dichlorophenyl)-6-benzoxazole carboxylic acid; tafamidisum

Appearance: White to off-white powder

Formulation:

CAS Number: 594839-88-0

Structure Available?: TRUE

Peptide sequence:

Salt Form: FALSE

Molecular Formula: C₁₄H₇Cl₂NO₃

Molecular Weight: 308.1

Cell-Permeable?: TRUE

Purity: >98%

Solubilities: ~1 mg/ml in ethanol, ~5 mg/ml in DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: Apotent kinetic stabilizer of transthyretin

MDL Number: MFCD16621109

PubChem CID: 11001318

SMILES: C1=CC2=C(C=C1C(=O)O)OC(=N2)C3=CC(=CC(=C3)Cl)Cl

InChi: InChI=1S/C14H7Cl2NO3/c15-9-3-8(4-10(16)6-9)13-17-11-2-1-7(14(18)19)5-12(11)20-13/h1-6H,(H,18,19)

InChi Key: TXEIIPDJKFWEEC-UHFFFAOYSA-N