Product Overview
Tafamidis | T4565 | TargetMol Chemicals
CAS: 594839-88-0
Smiles: OC(=O)c1ccc2nc(oc2c1)-c1cc(Cl)cc(Cl)c1
Formula: C14H7Cl2NO3
Pathway: Others
Target: Others
Receptor: N/A
Bioactivity: 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.
Molecular Weight: 308, 11
