Description
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.
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
Additional Information
Storage Condition: |
-20ºC |
Shipping Condition: |
RT |
Shelf Life: |
36 months |