DESCRIPTION
Synonyms
Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs.1 It binds to TTR with negative cooperativity (Kd1 = 3 nM; Kd2 = 278 nM) to stabilize the TTR dimer-dimer interface and inhibit tetrameric dissociation. Tafamidis stabilizes wild-type and clinically significant V30M and V122I mutant TTR amyloidogenic homotetramers (EC50s = 2.7-3.2 M) under fibril-promoting, denaturing, and physiological conditions in vitro. It stabilizes TTR heterotetramers containing wild-type and mutant subunits ex vivo in human plasma derived from patients carrying V30M or V1221 mutations when used at a concentration of 7.2 M. Formulations containing tafamidis have been used for the treatment of familial amyloid polyneuropathy.2
TECHNICAL INFORMATION
Formal Name
2-(3,5-dichloro
CAS Number
594839-88-0
Synonyms
Molecular Formula
C14H7Cl2NO3
Formula Weight
308.1
Purity
98%
Formulation
A crystalline solid
SHIPPING & STORAGE
-20C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
2 years
SR GROUP
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