Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 52.00 | |
10 mg | In stock | $ 85.00 | |
25 mg | In stock | $ 158.00 | |
50 mg | In stock | $ 239.00 | |
100 mg | In stock | $ 369.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 57.00 |
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) |
Synonyms | Fx-1006A |
Molecular Weight | 308.12 |
Formula | C14H7Cl2NO3 |
CAS No. | 594839-88-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 2 mg/mL
DMSO: 10 mg/mL (32.45 mM)
You can also refer to dose conversion for different animals. More
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Tafamidis 594839-88-0 Others Inhibitor Fx-1006A inhibit inhibitor