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Best price Fast Delivery 594839-88-0 Tafamidis Manufacturer CAS NO.594839-88-0
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Quick Details
- ProName: Best price Fast Delivery 594839-88-0 T...
- CasNo: 594839-88-0
- Molecular Formula: C14H7Cl2NO3
- Appearance: Powder or liquid
- Application: Medicinal Chemistry Biomedicine Phar...
- DeliveryTime: Goods in stock
- PackAge: According to customer
- Port: Shanghai
- ProductionCapacity: Metric Ton/Day
- Purity: 97%
- Storage: Store in a tightly closed container, i...
- Transportation: Fedex,DHL,TNT,BY SEA and BY AIR
- LimitNum: 10 Metric Ton
- Moisture Content: 5%
- Grade: Industrial Grade，Reagent Grade
Superiority
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
Tafamidis, Tafamidis, also known as Fx-1006 or PF-06291826, is a drug for the amelioration of transthyretin-related hereditary amyloidosis (also familial amyloid polyneuropathy, or FAP), a rare but deadly neurodegenerative disease. The drug was approved by the European Medicines Agency in November 2011 and by the Japanese Pharmaceuticals and Medical Devices Agency in September 2013. Tafamidis functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein.
Details
Tafamidis can be used as a benzoxole derivative that is a transthyretin (TTR) amyloid fibril inhibitors. It is a new drug candidate in the treatment of TTR amyloidosis (caused my misfolding of proteins).
Tafamidis is a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade. It is a drug for the amelioration of transthyretin-related hereditary amyloidosis. It functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein and binds selectively and with negative cooperativity to the two normally unoccupied thyroxine-binding sites of the tetramer, and kinetically stabilizes TTR.
Tafamidis(Fx1006A) is a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade.Target: OthersTafamidis is a drug for the amelioration of transthyretin-related hereditary amyloidosis.Tafamidis functions by kinetic stabilization of the correctly folded tetrameric form of the transthyretin (TTR) protein. Tafamidis binds selectively and with negative cooperativity (K(d)s ~2 nM and ~200 nM) to the two normally unoccupied thyroxine-binding sites of the tetramer, and kinetically stabilizes TTR. Patient-derived amyloidogenic variants of TTR, including kinetically and thermodynamically less stable mutants, are also stabilized by tafamidis binding. The crystal structure of tafamidis-bound TTR suggests that binding stabilizes the weaker dimer-dimer interface against dissociation, the rate-limiting step of amyloidogenesis