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Merck

219677

CFTR Inhibitor IV, PPQ-102

The CFTR Inhibitor IV, PPQ-102, also referenced under CAS 931706-15-9, controls the biological activity of CFTR. This small molecule/inhibitor is primarily used for Neuroscience applications.

Synonym(s):

CFTR Inhibitor IV, PPQ-102, 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

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About This Item

Empirical Formula (Hill Notation):
C26H22N4O3
CAS Number:
931706-15-9
Molecular Weight:
438.48
MDL number:
MFCD14824240
UNSPSC Code:
12352200
NACRES:
NA.28
Assay:
≥95% (HPLC)
Form:
crystalline solid
Quality level:
100
Storage condition:
OK to freeze
protect from light

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Product Name

CFTR Inhibitor IV, PPQ-102, The CFTR Inhibitor IV, PPQ-102, also referenced under CAS 931706-15-9, controls the biological activity of CFTR. This small molecule/inhibitor is primarily used for Neuroscience applications.

SMILES string

[n]21c(c5[n]([c]([n]([c](c5c2c6ccccc6)=O)C)=O)C)C(Nc4c1cccc4)c3[o]c(cc3)C

InChI

1S/C26H22N4O3/c1-15-13-14-19(33-15)21-24-23-20(25(31)29(3)26(32)28(23)2)22(16-9-5-4-6-10-16)30(24)18-12-8-7-11-17(18)27-21/h4-14,21,27H,1-3H3

InChI key

MNOOVRNGPIWJDI-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

crystalline solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

Related Categories

Disclaimer

Toxicity: Standard Handling (A)

Other Notes

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

Packaging

Packaged under inert gas

Legal Information

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

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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