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Tafamidis is a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade, with EC50s of 2.7-3.2 μM to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR. Tafamidis binds selectively and with negative cooperativity (K(d)s ~2 nM and ~200 nM) to the two normally unoccupied thyroxine-binding sites of the tetramer, and kinetically stabilizes TTR. Patient-derived amyloidogenic variants of TTR, including kinetically and thermodynamically less stable mutants, are also stabilized by tafamidis binding. The crystal structure of tafamidis-bound TTR suggests that binding stabilizes the weaker dimer-dimer interface against dissociation, the rate-limiting step of amyloidogenesis.
| Molecular Weight | 308.12 |
| Formula | C14H7Cl2NO3 |
| CAS Number | 594839-88-0 |
| Solubility (25°C) | DMSO 38 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Scott LJ. Drugs. Tafamidis: a review of its use in familial amyloid polyneuropathy.
| Related Transthyretin (TTR) Products |
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| A 1120
A 1120 is a high-affinity antagonist of retinol-binding protein 4 (RBP4) with a Ki value of 8.3 nM that disrupts the interaction between RBP4 and its conjugate transthyretin. |
| Acoramidis hydrochloride
Acoramidis (AG10) hydrochloride is an orally active, selective stabilizer of the thyroxine transporter (TTR (transthyretin)) that is effective against both wild-type and V1221 mutant types. Acoramidis (AG10) hydrochloride can be used for the study of transthyroxine amyloidosis. |
| Acoramidis
Acoramidis (AG10) is an orally active, selective stabilizer of the thyroxine transporter (TTR) that is effective against both wild-type and V1221 mutant types. |
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Products are for research use only. Not for human use. We do not sell to patients.
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