1. Membrane Transporter/Ion Channel
  2. CFTR
  3. PG01

PG01 

Cat. No.: HY-103369 Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

PG01 Chemical Structure

PG01 Chemical Structure

CAS No. : 853138-65-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 445 In-stock
Estimated Time of Arrival: December 31
1 mg USD 155 In-stock
Estimated Time of Arrival: December 31
5 mg USD 460 In-stock
Estimated Time of Arrival: December 31
10 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

CFTR[1]

In Vitro

PG01 itself does not activate ∆F508-CFTR, produces substantial ∆F508-CFTR Cl- current after the addition of 0.5 and 2 μM Forskolin. PG01 at 100 nM strongly stimulates channel activity with multiple channel openings observed. The apparent Kd for PG01 for G551D-CFTR activation is 1 μM, approximately 100-fold better than that of genistein. The potency for activation G1349D-CFTR by PG01 is even better at 40 nM. PG01 produces large currents in both G551D- and G1349D-CFTR expressing cells. The currents are sensitive to CFTRinh-172 and are not seen in nontransfected cells[1].

In Vivo

Pharmacokinetic analysis of PG01 in rats is done by serial measurements of plasma concentrations after single bolus infusions (5 mg/kg). PG01 pharmacokinetics fitted a two-compartment model with half-times of <5 min and 130 min with volume of distribution 4 L. Microsome metabolism studies and rat pharmacokinetic analysis suggests significantly more rapid metabolism of PG01 than SF-03[1].

Molecular Weight

439.55

Formula

C₂₈H₂₉N₃O₂

CAS No.

853138-65-5

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >98.0%

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Keywords:

PG01PG 01PG-01CFTRCystic fibrosis transmembrane conductance regulatorCysticfibrosisCl-channelpotentiatorforskolin-activatedcurrentE193KG970RcAMPInhibitorinhibitorinhibit

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PG01
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