PG 01

Cat. No. 3943

PG 01 C28H29N3O2 [853138-65-5]

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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 (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

Soluble to 100 mM in DMSO
>98 %
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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

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

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Keywords: PG 01, supplier, PG01, CTFR, mutant, potentiators, cystic, fibrosis, transmembrane, conductance, channels, CFTR, chloride, Cl-, pharmacochaperones, Tocris Bioscience, CFTR products

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