Tafamidis

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.Formal Name: 2-(3,5-dichlorophenyl)-6-benzoxazolecarboxylic acid. CAS Number: 594839-88-0. Synonyms: PF-06291826. Molecular Formula: C14H7Cl2NO3. Formula Weight: 308.1. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 214, 301, 310, 324 nm. SMILES: ClC1=CC(Cl)=CC(C(O2)=NC3=C2C=C(C(O)=O)C=C3)=C1. InChi Code: InChI=1S/C14H7Cl2NO3/c15-9-3-8(4-10(16)6-9)13-17-11-2-1-7(14(18)19)5-12(11)20-13/h1-6H,(H,18,19). InChi Key: TXEIIPDJKFWEEC-UHFFFAOYSA-N.