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Ivacaftor Chemical Structure

Ivacaftor

Data Sheet For research use only. Not for human use.
Cat. No. :BCP01857CAS No. :873054-44-5Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 873054-44-5 Cat. No. BCP01857
Name Ivacaftor
Synonyms VX-770;VX770;VX 770;Kalydeco;
SMILES
Chemical Name
Formula C24H28N2O3 M. Wt 392.49
Purity 98% Storage Store at 4-8°C
Description Ivacaftor (10 μM) significantly increases the forskolin-stimulated Cl- secretion (IT) by ~4-fold with an EC50 of 100 nM in the recombinant Fisher rat thyroid (FRT) cells expressing G551D gating mutation of CFTR, and by ~6-fold with an EC50 of 25 nM in the recombinant cells expressing temperature-corrected F508del processing mutation of CFTR. Consistent with the increases in the forskolin-stimulated IT, Ivacaftor (10 μM) increases the open probability (Po) of G551D-, F508del-, and wild-type CFTR by ~6-fold, ~5-fold and ~2-fold, respectively, indicating that Ivacaftor acts directly on CFTR to increase its gating activity. In primary cultured human CF bronchial epithelia (HBE) carrying the G551D and F508del CFTR mutations, Ivacaftor (10 μM) potently increases the forskolin-stimulated IT by ~10-fold from 5% to a maximum level of 48% of that measured in non-CF HBE, with an EC50 of 236 nM displaying ~70-fold more potency compared with the commonly used CFTR potentiator genistein, which has a
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