A thiazolidinone that selectively blocks the CFTR channel (Ki = 300 nM) in a voltage-independent manner; prevents cholera toxin-induced fluid secretion in the small intestine

CFTR Inhibitor-172 – 10 mg

Brand:
Cayman
CAS:
307510-92-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

The cystic fibrosis (CF) gene encodes a cAMP-regulated chloride channel, the CF transmembrane conductance regulator (CFTR).{25612} CFTR Inhibitor-172 is a thiazolidinone that selectively blocks the CFTR channel (Ki = 300 nM) in a voltage-independent manner.{26516} It appears to directly modulate the gating of chloride at the channel and does not prevent elevation of cAMP or inhibit other pumps or channels.{26516,26514} In mice, CFTR inhibitor-172 prevents cholera toxin-induced fluid secretion in the small intestine, when given by intraperitoneal injection.{26516,25797} It slows cyst growth in animal models of polycystic kidney disease.{26515} As CFTR also modulates glutathione (GSH) efflux, CFTR inhibitor-172 can affect intracellular GSH concentration and reactive oxygen species balance.{26511,26512,26513}  

 

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Description

A thiazolidinone that selectively blocks the CFTR channel (Ki = 300 nM) in a voltage-independent manner; prevents cholera toxin-induced fluid secretion in the small intestine, when given by intraperitoneal injection; can affect intracellular GSH concentration and ROS balance

Formal name: 4-[[4-oxo-2-thioxo-3-[3-(trifluoromethyl)phenyl]-5-thiazolidinylidene]methyl]-benzoic acid

Synonyms:  CFTR(inh)-172|Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172

Molecular weight: 409.4

CAS: 307510-92-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Bacterial Diseases|Cholera||Research Area|Oxidative Stress & Reactive Species|Reactive Sulfur|Glutathione

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