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Tafamidis [594839-88-0]
T4565
Overview
- SupplierTargetMol Chemicals
- Product NameTafamidis [594839-88-0]
- Delivery Days Customer9
- CAS Number594839-88-0
- Category SupplierChemical
- CertificationResearch Use Only
- Chemical NameTafamidis
- Molecular FormulaC14H7Cl2NO3
- Molecular Weight308.12
- Scientific DescriptionTafamidis (Fx-1006A) 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 microM) 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 microM. Formulations containing tafamidis have been used for the treatment of familial amyloid polyneuropathy.
- Shelf life instruction3 years
- SMILESClC=1C=C(C=2OC=3C(N2)=CC=C(C(O)=O)C3)C=C(Cl)C1
- Storage Instruction-20°C
- UNSPSC12352200
References
- 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.Read more