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Description: CFTR potentiator; corrects F508del-CFTR conductance defect
Chemical Name: N-Methyl-N-[2-[[4-(1-Methylethyl)phenyl]amino]-2-1H-indole-3-acetamide
Purity: ≥98% (HPLC)
Biological Activity for PG 01
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 for PG 01
| M. Wt | 439.55 |
| Formula | C28H29N3O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 853138-65-5 |
| PubChem ID | 4695397 |
| InChI Key | PQAYCXMQTUEDRD-UHFFFAOYSA-N |
| Smiles | O=C(C(C2=CC=CC=C2)N(C)C(CC3=CNC4=C3C=CC=C4)=O)NC1=CC=C(C(C)C)C=C1 |
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.
Product Datasheets for PG 01
References for PG 01
References are publications that support the biological activity of the product.
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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Keywords: PG 01, PG 01 supplier, PG01, CTFR, mutant, potentiators, cystic, fibrosis, transmembrane, conductance, channels, CFTR, chloride, Cl-, pharmacochaperones, 3943, Tocris Bioscience
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