PG 01

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Cat.No. 3943 - PG 01 | C28H29N3O2 | CAS No. 853138-65-5
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)
Datasheet
Citations
Reviews
Literature

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

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.95 100

Preparing Stock Solutions

The following data is based on the product molecular weight 439.55. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.28 mL 11.38 mL 22.75 mL
5 mM 0.46 mL 2.28 mL 4.55 mL
10 mM 0.23 mL 1.14 mL 2.28 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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References

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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