CFTRinh-172
Ki: 0.3 to 5 μM for channel opening
The cystic fibrosis (CF) transmembrane regulator (CFTR) is a cAMP-activated Cl channel expressed in epithelial cells of the lung, intestine, pancreas, and other tissues, where it facilitates transepithelial fluid transport. CFTRinh-172 is a highly potent and selective CFTR inhibitor.
In vitro: CFTRinh-172 could reversibly inhibit CFTR short-circuit current in less than 2 minutes in a voltage-independent manner. Moreover, at concentrations fully inhibiting CFTR, CFTRinh-172 did not prevent elevation of cellular cAMP or inhibit non-CFTR Cl–channels, multidrug resistance protein-1, ATP-sensitive K+ channels, or a series of other transporters [2].
In vivo: A single ip injection of CFTRinh-172 (250 μg/kg) in mice reduced by more than 90% cholera toxin–induced fluid secretion in the small intestine over 6 hours. CFTRinh-172 may be useful in developing large-animal models of cystic fibrosis and reducing intestinal fluid loss in cholera and other secretory diarrheas [3].
Clinical trial: Up to now, CFTRinh-172 is still in the preclinical development stage.
Reference:
[1] Ma T, Thiagarajah JR, Yang H, Sonawane ND, Folli C, Galietta LJ, Verkman AS.? Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest. 2002 Dec;110(11):1651-8.
Storage | Store at -20°C |
M.Wt | 409.4 |
Cas No. | 307510-92-5 |
Formula | C18H10F3NO3S2 |
Solubility | ≥40.9 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 4-[(E)-[4-oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]methyl]benzoic acid |
SDF | Download SDF |
Canonical SMILES | C1=CC(=CC(=C1)N2C(=O)C(=CC3=CC=C(C=C3)C(=O)O)SC2=S)C(F)(F)F |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment [1]: | |
Cell lines |
Fischer rat thyroid cells expressing human wild-type CFTR |
Preparation method |
The solubility of this compound in DMSO is >20.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
1 mM |
Applications |
CFTRinh-172 inhibited cAMP/flavone-stimulated Cl– transport in epithelial cells expressing CFTR. |
Animal experiment [1]: | |
Animal models |
Mice |
Dosage form |
250 μg/kg intraperitoneally |
Application |
A single administration of CFTRinh-172 prior to cholera toxin infusion effectively prevented fluid accumulation in the toxin-treated intestinal loops. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Ma T, Thiagarajah JR, Yang H, Sonawane ND, Folli C, Galietta LJ, Verkman AS. Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest. 2002 Dec;110(11):1651-8. |
Quality Control & MSDS
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