PG01

PG01 is a potent CFTR Cl- channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM) . PG01 increases ΔF508-CFTR Cl- current after adding Forskolin[1][2].

Product Specifications

CAS Number

[853138-65-5]

UNSPSC

12352005

Hazard Statement

H302, H413

Target

CFTR

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Endocrinology

Assay Protocol

https://www.medchemexpress.com/pg01.html

Concentration

10mM

Purity

98.04

Solubility

DMSO : 43.96 mg/mL (ultrasonic)

Smiles

O=C(N(C)C(C1=CC=CC=C1)C(NC2=CC=C(C(C)C)C=C2)=O)CC3=CNC4=C3C=CC=C4

Molecular Formula

C28H29N3O2

Molecular Weight

439.55

Precautions

H302, H413

References & Citations

[1]Pedemonte N, et al. Phenylglycine and sulfonamide correctors of defective delta F508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating. Mol Pharmacol. 2005 May;67 (5) :1797-807.|[2]Caputo A, et al. Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators. J Pharmacol Exp Ther. 2009 Sep;330 (3) :783-91.