Tafamidis

Modify Date: 2024-01-04 20:54:58

Tafamidis Structure
Tafamidis structure
 Common Name Tafamidis
CAS Number 594839-88-0 Molecular Weight 308.116
Density 1.5±0.1 g/cm3 Boiling Point 486.7±40.0 °C at 760 mmHg
Molecular Formula C14H7Cl2NO3 Melting Point N/A
MSDS N/A Flash Point 248.1±27.3 °C

 Use of Tafamidis


Tafamidis(Fx1006A) is a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade.Target: OthersTafamidis is a drug for the amelioration of transthyretin-related hereditary amyloidosis.Tafamidis functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein. 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 [1].

 Names

Name tafamidis
Synonym More Synonyms

 Tafamidis Biological Activity

Description Tafamidis(Fx1006A) is a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade.Target: OthersTafamidis is a drug for the amelioration of transthyretin-related hereditary amyloidosis.Tafamidis functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein. 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 [1].
Related Catalog
References

[1]. Bulawa, C.E., et al., Tafamidis, a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade. Proc Natl Acad Sci U S A, 2012. 109(24): p. 9629-34.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 486.7±40.0 °C at 760 mmHg
Molecular Formula C14H7Cl2NO3
Molecular Weight 308.116
Flash Point 248.1±27.3 °C
Exact Mass 306.980286
PSA 63.33000
LogP 5.29
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.677
Storage condition 2-8℃

 Synonyms

6-Benzoxazolecarboxylic acid, 2-(3,5-dichlorophenyl)-
Tafamidis
8FG9H9D31J
2-(3,5-Dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid
UNII-8FG9H9D31J
FX-1006
3MI
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