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Purity: ≥98%
Tafamidis meglumine (formerly Fx-1006; PF-06291826; Vyndaqel and Vyndamax), the meglumine salt of tafamidis, is a potent and selective
transthyretin (TTR) stabilizer, is an approved drug for the amelioration of
transthyretin-related hereditary amyloidosis (also familial amyloid
polyneuropathy, or FAP), a rare but deadly neurodegenerative disease. It
shows comparable potency and efficacy to the mutumant homotetramers
V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM.
Tafamidis inhibits amyloidogenesis. 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.
| ln Vitro |
Tafamidis kinetically stabilizes TTR by inertly binding the two common polarin sites of the tetramer with negative affinity (Kds ∼2 nM and ∼200 nM) [1]. After 72 hours at pH 4.4-4.5, tacramamide (0-7.2 μM) quantitatively suppresses WT-TTR amyloidosis [1].
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| References |
[1]. Bulawa CE, et al. Tafamidis, a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade. Proc Natl Acad Sci U S A. 2012 Jun 12;109(24):9629-34.
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| Molecular Formula |
C21H24CL2N2O8
|
|---|---|
| Molecular Weight |
503.329864501953
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| CAS # |
951395-08-7
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| Related CAS # |
Tafamidis;594839-88-0
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| SMILES |
OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CNC.O=C(C1=CC=C2N=C(C3=CC(Cl)=CC(Cl)=C3)OC2=C1)O
|
| InChi Key |
DQJDBUPLRMRBAB-WZTVWXICSA-N
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| InChi Code |
InChI=1S/C14H7Cl2NO3.C7H17NO5/c15-9-3-8(4-10(16)6-9)13-17-11-2-1-7(14(18)19)5-12(11)20-131-8-2-4(10)6(12)7(13)5(11)3-9/h1-6H,(H,18,19)4-13H,2-3H2,1H3/t4-,5+,6+,7+/m.0/s1
|
| Chemical Name |
(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentaol 2-(3,5-dichlorophenyl)benzo[d]oxazole-6-carboxylic acid
|
| Synonyms |
Fx 1006A PF-06291826Fx-1006A PF 06291826Fx1006A PF06291826
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~24.83 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.48 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9868 mL | 9.9338 mL | 19.8677 mL | |
| 5 mM | 0.3974 mL | 1.9868 mL | 3.9735 mL | |
| 10 mM | 0.1987 mL | 0.9934 mL | 1.9868 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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