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Merck
모든 사진(1)

주요 문서

219670

Sigma-Aldrich

CFTR Inhibitor-172

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

동의어(들):

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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About This Item

실험식(Hill 표기법):
C18H10F3NO3S2
CAS Number:
Molecular Weight:
409.40
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

제품명

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).

Quality Level

분석

≥95% (HPLC)

양식

solid

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

색상

yellow

solubility

DMSO: 5 mg/mL

배송 상태

ambient

저장 온도

2-8°C

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

일반 설명

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).

생화학적/생리학적 작용

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

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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.

법적 정보

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3


시험 성적서(COA)

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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
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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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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

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