Drug intelligence / Profile preview

CFTR-Inh172

Development stage
Preclinical
Modality
Small Molecules
01

Overview

CFTR-Inh172 is a potent, selective, and voltage-independent inhibitor of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. Discovered by Alan Verkman's laboratory at the University of California, San Francisco (UCSF) through high-throughput screening, the compound acts as a gating inhibitor by binding to the pore of the CFTR channel and stabilizing its closed state, thereby preventing chloride ion transport. It is widely utilized as a research tool to study CFTR function in vitro and in vivo, and has been investigated in preclinical models for potential therapeutic applications in secretory diarrheas (such as cholera) and polycystic kidney disease.

Other names
4-[[(5Z)-4-oxo-2-thioxo-3-[3-(trifluoromethyl)phenyl]-5-thiazolidinylidene]methyl]benzoic acid4-[(Z)-[4-oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]methyl]benzoic acidCFTR inhibitor 172CFTR Inhibitor-172
02

Targets

ORAI1 (Calcium release–activated calcium channel protein 1)CFTR (Cystic fibrosis transmembrane conductance regulator)

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