Ataluren
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Ataluren
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CAS No:
775304-57-9
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Formula:
C15H9FN2O3
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Chemical Name:
Ataluren
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Synonyms:
Benzoic acid,3-[5-(2-fluorophenyl)-1,2,4-oxadiazol-3-yl]-;3-[5-(2-Fluorophenyl)-1,2,4-oxadiazol-3-yl]benzoic acid;PTC 124;Ataluren;PCT 124;Translarna;918899-30-6
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CAS No:
Ataluren Use and Manufacturing
Nonsense mutations create a premature termination of mRNA translation and have been implicated in various genetic disorders, including muscular dystrophy and cystic fibrosis. PTC-124 is a nonaminoglycoside that has been reported to selectively induce ribosomes to read through premature nonsense stop signals on mRNA, thus allowing the production of full-length, functional proteins. In a mouse model of cystic fibrosis caused by nonsense mutations, PTC-124 treatment (60 mg/kg s.c. injection or 0.3-0.9 mg/ml orally) has been shown to restore cystic fibrosis transmembrane conductance regulator (CFTR) protein expression and function. The target activity of PTC-124 was initially evaluated by firefly luciferase reporter cell-based nonsense codon assay (IC50 = 7 nM); however, subsequent assessments using a Renilla reniformis luciferase reporter have failed to produce nonsense codon suppression activity. Thus, while PTC-124 is in clinical testing in patients with nonsense mutations within the CFTR or dystrophin genes, controversy surrounds its exact mechanism of action.[Cayman Chemical]
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