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Merck

219670

CFTR Inhibitor-172

≥95% (HPLC), solid, CFTR inhibitor, Calbiochem®

Synonyme(s) :

CFTR Inhibitor-172, 3-[(3-Trifluoromethyl)phenyl]-5-[(4-carboxyphenyl)methylene]-2-thioxo-4-thiazolidinone, CFTR inh-172, 3-[(3-Trifluoromethyl)phenyl]-5-[(4-carboxyphenyl)methylene]-2-thioxo-4-thiazolidinone, CFTRinh-172

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A propos de cet article

Formule empirique (notation de Hill) :
C18H10F3NO3S2
Numéro CAS:
307510-92-5
Poids moléculaire :
409.40
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD06411408
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light

Principaux documents

Voir toute la documentation
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Nom du produit

CFTR Inhibitor-172, CFTR Inhibitor-172, CAS 307510-92-5, is a cell-permeable, potent, reversible, rapid, and voltage-independent inhibitor of CFTR-mediated Cl- transport in human airway cells (Ki ~ 300 nM).

storage condition

OK to freeze, protect from light

SMILES string

FC(F)(F)c1cc(ccc1)N2C(=S)S\C(=C/c3ccc(cc3)C(=O)O)\C2=O

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-ZSOIEALJSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

color

yellow

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Catégories apparentées

General description

A cell-permeable 2-thio-4-thiazolidinone compound that acts as a potent, reversible, rapid, and voltage-independent inhibitor of CFTR (cystic fibrosis transmembrane conductance regulator)-mediated Cl- transport in human airway cells (Ki ~ 300 nM). It does not prevent elevation of cellular cAMP, nor does it inhibit non-CFTR Cl- channels, MDR-1, ATP-sensitive K+ channels, or a series of other transporters even at concentrations as high as 5 µM. Shown to block cholera toxin-induced intestinal fluid secretion in mice. May be also useful for reducing intestinal fluid loss in other secretory diarrheas. Also available as a 50 mM solution in DMSO (Cat. No. 219674).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
CFTR
Product does not compete with ATP.
Reversible: yes
Target Ki: ~ 300 nM against CFTR (cystic fibrosis transmembrane conductance regulator)-mediated Cl- transport in human airway cells

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Yang, H., et al. 2003. J. Biol. Chem.278, 35079.
Al-Awqati, Q., et al. 2002. J. Clin. Invest.110, 1599.
Ma, T., et al. 2002. J. Clin. Invest.110, 1651.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

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Pawin Pongkorpsakol et al.
Journal of experimental pharmacology, 15, 449-466 (2023-11-29)
Inhibition of Ca2+-activated transmembrane protein 16A (TMEM16A) Cl- channels has been proposed to alleviate mucus secretion in asthma. In this study, we identified a novel class of TMEM16A inhibitors from natural sources in airway epithelial Calu-3 cells and determine anti-asthmatic
Maite Calucho et al.
Scientific reports, 11(1), 15511-15511 (2021-08-01)
The availability of a simple, robust and non-invasive in vitro airway model would be useful to study the functionality of the cystic fibrosis transmembrane regulator (CFTR) protein and to personalize modulator therapy for cystic fibrosis (CF) patients. Our aim was
Guadalupe Ortiz-Muñoz et al.
The Journal of clinical investigation, 130(4), 2041-2053 (2020-01-22)
Cystic fibrosis (CF) lung disease is characterized by an inflammatory response that can lead to terminal respiratory failure. The cystic fibrosis transmembrane conductance regulator (CFTR) is mutated in CF, and we hypothesized that dysfunctional CFTR in platelets, which are key

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