PG 01
Chemical Name: N-Methyl-N-[2-[[4-(1-Methylethyl)phenyl]amino]-2-1H-indole-3-acetamide
Purity: ≥98%
Biological Activity
Cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. Corrects gating defects of CFTR mutants such as ΔF508 (Ka = 0.3 μM), E193K and G970R (Kd values are 0.22 μM and 0.45 μM respectively). Increases ΔF508-CFTR Cl- currents in the presence of forskolin; displays no effect on Ca2+-activated Cl- current.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Phenylglycine and sulphonamide correctors of defective DF508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating.
Pedemonte et al.
Mol.Pharmacol., 2005;67:1797 -
Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators.
Caputo et al.
J.Pharmacol.Exp.Ther., 2009;330:783 -
Influence of cell background on pharmacological rescue of mutant CFTR.
Pedemonte et al.
Am.J.Physiol.Cell Physiol, 2010;298:C866
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