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C2992

Sigma-Aldrich

CFTR Inhibitor-172

≥98% (HPLC), powder, CFTR inhibitor

Synonym(s):

5-[(4-Carboxyphenyl)methylene]-2-thioxo-3-[(3-trifluoromethyl)phenyl-4-thiazolidinone

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About This Item

Empirical Formula (Hill Notation):
C18H10F3NO3S2
CAS Number:
307510-92-5
Molecular Weight:
409.40
MDL number:
MFCD06411408
UNSPSC Code:
12352200
PubChem Substance ID:
24724436
NACRES:
NA.77

product name

CFTR(inh)-172, ≥98% (HPLC), powder

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

yellow

solubility

DMSO: ≥10 mg/mL
H2O: insoluble

storage temp.

2-8°C

SMILES string

OC(=O)c1ccc(cc1)\C=C2\SC(=S)N(C2=O)c3cccc(c3)C(F)(F)F

InChI

1S/C18H10F3NO3S2/c19-18(20,21)12-2-1-3-13(9-12)22-15(23)14(27-17(22)26)8-10-4-6-11(7-5-10)16(24)25/h1-9H,(H,24,25)/b14-8+

InChI key

JIMHYXZZCWVCMI-RIYZIHGNSA-N

Application

CFTR(inh)-172 has been used to specifically inhibit cystic fibrosis transmembrane conductance regulator (CFTR) activity. It is also used as a CFTR inhibitor Inh-172 to treat forskolin and IBMX.

Biochem/physiol Actions

CFTR(inh)-172 is an inhibitor of the cystic fibrosis transmembrane conductance regulator (CFTR). With a Ki = 300 nM,. CFTR(inh)-172 leads to rapid, reversible and voltage-independent inhibition; it is an antidiarrheal agent in animals. CTFR(inh)-172 may be a useful tool to study animal models of cystic fibrosis and intestinal fluid loss in cholera and other secretory diarrheas. CTFR(inh)-172 is structurally-unrelated to known, but non-specific CFTR inhibitors DPC, NPPB (Cat. No. N4779) and Glibenclamide.

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Storage Class

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Certificates of Analysis (COA)

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An unexpected effect of TNF-alpha on F508del-CFTR maturation and function
Bitam S, et al.
F1000Research, 4 (2015)
Defective CFTR expression and function are detectable in blood monocytes: development of a new blood test for cystic fibrosis
Sorio C, et al.
Testing, 6(7), e22212-e22212 (2011)
Electrophysiological evaluation of cystic fibrosis conductance transmembrane regulator (CFTR) expression in human monocytes
Ettorre M, et al.
Biochimica et biophysica acta. General subjects, 1840(10), 3088-3095 (2014)
N D Sonawane et al.
Journal of pharmaceutical sciences, 94(1), 134-143 (2005-03-12)
A small-molecule inhibitor of the cystic fibrosis transmembrane conductance regulator (CFTR), 3-[(3-trifluoromethyl)phenyl]-5-[(4-carboxyphenyl)methylene]-2-thioxo-4-thiazolidinone (CFTR(inh)-172), reduces enterotoxin-induced intestinal fluid secretion in rodents. Here, we study CFTR(inh)-172 pharmacology and antidiarrheal efficacy in rodents using (14)C-labeled CFTR(inh)-172, liquid chromatography/mass spectrometry, and a closed intestinal
Tonghui Ma et al.
The Journal of clinical investigation, 110(11), 1651-1658 (2002-12-05)
Secretory diarrhea is the leading cause of infant death in developing countries and a major cause of morbidity in adults. The cystic fibrosis transmembrane conductance regulator (CFTR) protein is required for fluid secretion in the intestine and airways and, when
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