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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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Pricing

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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)
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)
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
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