2. Membrane Transporter/Ion Channel
  3. CFTR
  4. 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.

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PG01 Chemical Structure

PG01 Chemical Structure

CAS No. : 853138-65-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 445 In-stock
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10 mM * 1 mL in DMSO USD 445 In-stock
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5 mg USD 460 In-stock
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Based on 1 publication(s) in Google Scholar

PG01 Related Antibodies

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PG01 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

439.55

Formula

C28H29N3O2
CAS No.
Appearance

Solid

Color

White to off-white

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
Solvent & Solubility
In Vitro: 

DMSO : 43.96 mg/mL (100.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2751 mL 11.3753 mL 22.7505 mL
5 mM 0.4550 mL 2.2751 mL 4.5501 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥98.0%

COA (248 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2751 mL 11.3753 mL 22.7505 mL 56.8764 mL
5 mM 0.4550 mL 2.2751 mL 4.5501 mL 11.3753 mL
10 mM 0.2275 mL 1.1375 mL 2.2751 mL 5.6876 mL
15 mM 0.1517 mL 0.7584 mL 1.5167 mL 3.7918 mL
20 mM 0.1138 mL 0.5688 mL 1.1375 mL 2.8438 mL
25 mM 0.0910 mL 0.4550 mL 0.9100 mL 2.2751 mL
30 mM 0.0758 mL 0.3792 mL 0.7584 mL 1.8959 mL
40 mM 0.0569 mL 0.2844 mL 0.5688 mL 1.4219 mL
50 mM 0.0455 mL 0.2275 mL 0.4550 mL 1.1375 mL
60 mM 0.0379 mL 0.1896 mL 0.3792 mL 0.9479 mL
80 mM 0.0284 mL 0.1422 mL 0.2844 mL 0.7110 mL
100 mM 0.0228 mL 0.1138 mL 0.2275 mL 0.5688 mL
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PG01 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PG01853138-65-5PG 01PG-01CFTRCystic fibrosis transmembrane conductance regulatorCysticfibrosisCl-channelpotentiatorforskolin-activatedcurrentE193KG970RcAMPInhibitorinhibitorinhibit

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