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Merck
CN
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219677

Sigma-Aldrich

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.

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别名:
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
经验公式(希尔记法):
C26H22N4O3
分子量:
438.48
UNSPSC代码:
12352200
NACRES:
NA.28

质量水平

检测方案

≥95% (HPLC)

形式

crystalline solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

white

溶解性

DMSO: 5 mg/mL

运输

ambient

储存温度

−20°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

一般描述

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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他说明

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

法律信息

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

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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