Tafamidis-d3

Description: Tafamidis-d3 is a deuterated compound of Tafamidis. Tafamidis has a CAS number of 594839-88-0. Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs. 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 µM) 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 µM. Formulations containing tafamidis have been used for the treatment of familial amyloid polyneuropathy. Smiles: O=C(C1=C([2H])C([2H])=C2N=C(C3=CC(Cl)=CC(Cl)=C3)OC2=C1[2H])O