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Chemical Structure| 931706-15-9 Chemical Structure| 931706-15-9

Structure of PPQ-102
CAS No.: 931706-15-9

Chemical Structure| 931706-15-9

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PPQ-102 is a potent and voltage-independent CFTR inhibitor, which completely inhibit CFTR chloride current with IC50 approximately 90 nM.

Synonyms: CFTR Inhibitor; Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor IV; CFTR Inhibitor IV

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Product Details of PPQ-102

CAS No. :931706-15-9
Formula : C26H22N4O3
M.W : 438.48
SMILES Code : CC1=CC=C(C2C3=C(C4=C(N3C5=C(N2)C=CC=C5)C6=CC=CC=C6)N(C)C(N(C4=O)C)=O)O1
Synonyms :
CFTR Inhibitor; Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor IV; CFTR Inhibitor IV
MDL No. :MFCD14824240
InChI Key :MNOOVRNGPIWJDI-UHFFFAOYSA-N
Pubchem ID :16016583

Safety of PPQ-102

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H317
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
NPTr cells 30 µM 2 hours Inhibition of VRAC activity, reducing CDT-induced apoptosis in NPTr cells Virulence. 2023 Dec;14(1):2287339
CFBE41o- WT cells 0.1, 1, 5, 10, 20, 30 µM 48 hours To evaluate the anti-SARS-CoV-2 activity of PPQ-102. Results showed that PPQ-102 inhibited SARS-CoV-2 replication by nearly 100% at 30 μM, with an IC50 of 15.92 μM. Cells. 2023 Feb 28;12(5):776
HEK-293 cells 10 µM and 30 µM 5 minutes Test the inhibitory effect of PPQ-102 on VRAC/LRRC8-mediated chloride conductance, with an IC50 value of 19.6±1.5 μM Front Pharmacol. 2017 May 31;8:328

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Polycystic kidney disease model Added to culture medium 0.5 µM, 2.5 µM, 5 µM Medium replaced every 12 hours for 4 days Evaluating PPQ-102 inhibition of cyst formation, 0.5 μM PPQ-102 inhibited cyst formation by ~60%, and 2.5 μM and 5 μM PPQ-102 nearly completely inhibited cyst formation. J Med Chem. 2009 Oct 22;52(20):6447-55

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.40mL

2.28mL

1.14mL

22.81mL

4.56mL

2.28mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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