1. Membrane Transporter/Ion Channel
  2. CFTR
  3. PPQ-102

PPQ-102  (Synonyms: CFTR Inhibitor)

Cat. No.: HY-14179 Purity: 99.82%
COA Handling Instructions

PPQ-102 (CFTR Inhibitor) is a reversible CFTR inhibitor that completely inhibits CFTR chloride currents (IC50 ~90 nM). PPQ-102 is not affected by membrane potential-dependent cell allocation or blocking efficiency (uncharged at physiological pH) and effectively prevents cyst enlargement in polycystic kidney disease.

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

PPQ-102 Chemical Structure

PPQ-102 Chemical Structure

CAS No. : 931706-15-9

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
5 mg USD 96 In-stock
10 mg USD 168 In-stock
50 mg USD 660 In-stock
100 mg USD 1020 In-stock
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500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PPQ-102 (CFTR Inhibitor) is a reversible CFTR inhibitor that completely inhibits CFTR chloride currents (IC50 ~90 nM). PPQ-102 is not affected by membrane potential-dependent cell allocation or blocking efficiency (uncharged at physiological pH) and effectively prevents cyst enlargement in polycystic kidney disease[1].

IC50 & Target

IC50: ~90 nM (CFTR)[1].

In Vitro

PPQ-102 (0, 0.5, 5μM, 4 days) prevents and reverses renal cyst expansion in an embryonic kidney organ culture model of PKD[1].
PPQ-102 (0, 0.5, 5μM, 3 days) shows ability of reducing fluid accumulation in preformed cysts[1].

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

Cell Viability Assay[1]

Cell Line: E13.5 embryonic kidneys (embryonic kidney organ culture model of PKD)
Concentration: 0, 0.5, 5 μM
Incubation Time: 3 or 4 days
Result: Remarkablyreduced the number and size of renal cysts formed in the 8-Br-cAMP-containing medium (showed ∼60% inhibition of cyst formation at 0.5 μM, near complete absence of cysts at 2.5 and 5 μM).
Remarkable reduced cyst size over 1 and 2 days in the 8-Br-cAMP-containing medium.
Molecular Weight

438.48

Formula

C26H22N4O3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CN1C(C2=C(C3=CC=CC=C3)N4C5=CC=CC=C5NC(C6=CC=C(C)O6)C4=C2N(C)C1=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (114.03 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 2.2806 mL 11.4030 mL 22.8061 mL
5 mM 0.4561 mL 2.2806 mL 4.5612 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.70 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2806 mL 11.4030 mL 22.8061 mL 57.0151 mL
5 mM 0.4561 mL 2.2806 mL 4.5612 mL 11.4030 mL
10 mM 0.2281 mL 1.1403 mL 2.2806 mL 5.7015 mL
15 mM 0.1520 mL 0.7602 mL 1.5204 mL 3.8010 mL
20 mM 0.1140 mL 0.5702 mL 1.1403 mL 2.8508 mL
25 mM 0.0912 mL 0.4561 mL 0.9122 mL 2.2806 mL
30 mM 0.0760 mL 0.3801 mL 0.7602 mL 1.9005 mL
40 mM 0.0570 mL 0.2851 mL 0.5702 mL 1.4254 mL
50 mM 0.0456 mL 0.2281 mL 0.4561 mL 1.1403 mL
60 mM 0.0380 mL 0.1901 mL 0.3801 mL 0.9503 mL
80 mM 0.0285 mL 0.1425 mL 0.2851 mL 0.7127 mL
100 mM 0.0228 mL 0.1140 mL 0.2281 mL 0.5702 mL
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PPQ-102 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.

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Product Name:
PPQ-102
Cat. No.:
HY-14179
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