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219670

Sigma-Aldrich

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).

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别名:
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
经验公式(希尔记法):
C18H10F3NO3S2
分子量:
409.40
MDL编号:

质量水平

检测方案

≥95% (HPLC)

形式

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

yellow

溶解性

DMSO: 5 mg/mL

运输

ambient

储存温度

2-8°C

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

一般描述

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.
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).

生化/生理作用

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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.

法律信息

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

储存分类代码

11 - Combustible Solids

WGK

WGK 3


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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
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
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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