Chemical Property of Tafamidis
Chemical Property:
- Boiling Point:486.7±40.0 °C(Predicted)
- PKA:3.49±0.30(Predicted)
- PSA：63.33000
- Density:1.530
- LogP:4.49980
- Storage Temp.:-20°
- Solubility.:Soluble in DMSO (up to 20 mg/ml).
- XLogP3:4.2
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:2
- Exact Mass:306.9802985
- Heavy Atom Count:20
- Complexity:371
- Purity/Quality:
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99%, *data from raw suppliers
PF-06291826(Tafamidis) >98% *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:C1=CC2=C(C=C1C(=O)O)OC(=N2)C3=CC(=CC(=C3)Cl)Cl
- Recent ClinicalTrials:This Study Will Examine the Clinical Effectiveness of Tafamidis in Patients With Mixed Phenotype Hereditary Transthyretin Amyloidosis
- Recent EU Clinical Trials:A PHASE 3 MULTICENTER, OPEN-LABEL STUDY TO EVALUATE THE SAFETY OF DAILY ORAL DOSING OF
- Recent NIPH Clinical Trials:Pathophysiological impacts of tafamidis on cardiac transthyretin amyloidosis
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Description
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.
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Uses
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).
