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Chemical Structure| 307510-92-5 Chemical Structure| 307510-92-5

Structure of CFTR(inh)-172
CAS No.: 307510-92-5

Chemical Structure| 307510-92-5

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CFTR (inh)-172 is an reversibly inhibitor of CFTR short-circuit current in less than 2 minutes in a voltage-independent manner with Ki ~300 nM.

Synonyms: CFTR Inhibitor-172; Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172; CFTRinh-172

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Product Details of CFTR(inh)-172

CAS No. :307510-92-5
Formula : C18H10F3NO3S2
M.W : 409.40
SMILES Code : O=C1N(C2=CC=CC(C(F)(F)F)=C2)C(S/C1=C\C3=CC=C(C(O)=O)C=C3)=S
Synonyms :
CFTR Inhibitor-172; Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172; CFTRinh-172
MDL No. :MFCD01164609

Safety of CFTR(inh)-172

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H319-H372-H410
Precautionary Statements:P501-P273-P260-P270-P264-P280-P391-P314-P337+P313-P305+P351+P338-P301+P312+P330
Class:9
UN#:3077
Packing Group:

Isoform Comparison

Biological Activity

Target
  • CFTR

    CFTR, Ki:300 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Renal proximal cells (PCT cells) 5 µM 24 hours CFTR(inh)-172 prevents cisplatin-induced cell death and apoptosis by modulating the intracellular reactive oxygen species (ROS) balance and glutathione (GSH) concentration. Cell Death Dis. 2013 Oct 3;4(10):e817.
A549 cells 5 µM 24 hours CFTR(inh)-172 does not impair the antitumor activity of cisplatin in A549 cancer cells. Cell Death Dis. 2013 Oct 3;4(10):e817.
Human peripheral blood neutrophils 0.5, 1, 2.5, 5 µM 4 hours CFTR(inh)-172 increased CitH3 protein expression and dsDNA fluorescence staining in a concentration-dependent manner, indicating its promotion of NET formation. Acta Pharmacol Sin. 2022 Nov;43(11):2848-2861.
FRT cells 20 µM Inhibit CFTR channel activity and reverse the increase in Cl- current induced by anthraquinone compounds Acta Pharmacol Sin. 2011 Jun;32(6):834-9.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Cisplatin-induced nephrotoxicity model Intraperitoneal injection 1 mg/kg Single dose, 30 minutes before cisplatin injection CFTR(inh)-172 pretreatment significantly prevented cisplatin-induced nephrotoxicity, improved renal function, and reduced oxidative stress. Cell Death Dis. 2013 Oct 3;4(10):e817.
Mice Wild-type C57BL/6J mice Intravenous injection 2 mg/kg 24 hours CFTR(inh)-172 increased neutrophil [Cl?]i and dsDNA release, indicating its promotion of NET formation in vivo. Acta Pharmacol Sin. 2022 Nov;43(11):2848-2861.
SD rats Closed colonic loop model Intraperitoneal injection 40 µmol/L Single dose, lasted for 6 hours Inhibit fluid accumulation in the colon induced by rhein Acta Pharmacol Sin. 2011 Jun;32(6):834-9.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.43mL

4.89mL

2.44mL

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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