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219677

CFTR Inhibitor IV, PPQ-102

Name: CFTR Inhibitor IV, PPQ-102
Brand: MM

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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Properties

Quality Level

100

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

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

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.

Packaging

Packaged under inert gas

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c