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219677 Sigma-Aldrich

CFTR Inhibitor IV, PPQ-102 - CAS 931706-15-9 - Calbiochem

CFTR Inhibitor IV, PPQ-102, CAS 931706-15-9, is a cell-permeable inhibitor of CFTR-mediated chloride current in a reversible and voltage-independent manner.

Synonym: 7,9-Dimethyl-11-phenyl-6-(5-methylfuran-2-yl)-5,6-dihydro-pyrimido-[4ʹ,5ʹ-3,4]pyrrolo[1,2-a]quinoxaline-8,10-(7H,9H)-dione, Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor IV, 7,9-Dimethyl-11-phenyl-6-(5-methylfuran-2-yl)-5,6-dihydro-pyrimido-[4ʹ,5ʹ-3,4]pyrrolo[1,2-a]quinoxaline-8,10-(7H,9H)-dione, Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor IV

  • CAS Number 931706-15-9

  • Empirical Formula (Hill Notation) C26H22N4O3

  • Molecular Weight 438.48

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Properties

Related Categories Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology More...
packaging   10 mg in Glass bottle (219677-10MG)
color   white
form   crystalline solid
shipped in   ambient
solubility   DMSO: 5 mg/mL
storage condition   OK to freeze
  protect from light
brand family   Calbiochem
purity   ≥95% by HPLC
storage conditions   -20C

Description

General description

A cell-permeable pyrimido-pyrrolo-quinoxalinedione (PPQ) compound that targets the intracellular nucleotide binding domain(s) of CFTR and inhibits CFTR-mediated chloride current in a reversible and voltage-independent manner. Single channel recordings of CFTR-expressing FRT cells upon forskolin (Cat. No. 344270) and IBMX (Cat. No. 410957) stimulation indicate that the nature of PPQ-102 inhibition is due to a stabilization of the channels in a closed state (7.8- vs. 0.4-fold increase of mean channel close vs. open time, respectively, with 1 µM PPQ-102). PPQ-102 at 5 µM is shown to completely prevent Sp-8-Br-cAMP- (Cat. No. 116818) induced cysts formation and reduce the size of preformed cysts in an ex vivo murine neonatal kidney organ culture.

A cell-permeable pyrimido-pyrrolo-quinoxalinedione (PPQ) compound that targets the intracellular nucleotide binding domain(s) of CFTR and inhibits CFTR-mediated chloride current in a reversible and voltage-independent manner. Single channel recordings of CFTR-expressing FRT cells upon forskolin (Cat. No. 344270) and IBMX (Cat. No. 410957) stimulation indicate that the nature of PPQ-102 inhibition is due to a stabilization of the channels in a closed state (7.8- vs. 0.4-fold increase of mean channel close vs. open time, respectively, with 1 µM PPQ-102). PPQ-102 at 5 µM is shown to completely prevent Sp-8-Br-cAMP- (Cat. No. 116818) induced cysts formation and reduce the size of preformed cysts in an ex vivo murine neonatal kidney organ culture.

Other Notes

Tradtrantip, L., et al. 2009. J. Med. Chem.52, 6447.

Packaging

10 mg in Glass bottle

Packaged under inert gas

Warning

Standard Handling (A)

Safety & Documentation

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