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Tafamidis (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 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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $52 | In Stock | |
10 mg | $85 | In Stock | |
25 mg | $158 | In Stock | |
50 mg | $239 | In Stock | |
100 mg | $369 | In Stock | |
1 mL x 10 mM (in DMSO) | $57 | In Stock |
Description | Tafamidis (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 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. |
Targets&IC50 | TTR (WT, V30M, V122I):2.7-3.2 μM(ec50) |
Alias | Fx-1006A |
Molecular Weight | 308.12 |
Formula | C14H7Cl2NO3 |
Cas No. | 594839-88-0 |
Smiles | ClC=1C=C(C=2OC=3C(N2)=CC=C(C(O)=O)C3)C=C(Cl)C1 |
Relative Density. | 1.530 g/cm3 |
Storage | keep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 2 mg/mL DMSO: 19.23 mg/ml (62.41 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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