219670

CFTR Inhibitor-172

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

• Synonym(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, CFTR_inh-172
• Empirical Formula (Hill Notation): C₁₈H₁₀F₃NO₃S₂
• CAS Number: 307510-92-5
• Molecular Weight: 409.40
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD06411408
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Product Name: 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 (K_i ~ 300 nM).
• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: yellow
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: 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

Description

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 (K_i ~ 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 K_i: ~ 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)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3