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PG 01

Cat. No. 3943

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Chemical Name: N-Methyl-N-[2-[[4-(1-Methylethyl)phenyl]amino]-2-1H-indole-3-acetamide

Biological Activity

Cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. Corrects gating defects of CFTR mutants such as ΔF508 (K_a = 0.3 μM), E193K and G970R (K_d 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

M.Wt:

439.55

Formula:

C₂₈H₂₉N₃O₂

Solubility:

Soluble to 100 mM in DMSO

Purity:

>98 %

Storage:

Store at -20°C

CAS No:

853138-65-5

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Pedemonte et al (2005) Phenylglycine and sulphonamide correctors of defective DF508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating. Mol.Pharmacol. 67 1797. PMID: 15722457.

Caputo et al (2009) Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators. J.Pharmacol.Exp.Ther. 330 783. PMID: 19491324.

Pedemonte et al (2010) Influence of cell background on pharmacological rescue of mutant CFTR. Am.J.Physiol.Cell Physiol 298 C866. PMID: 20053923.

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