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.

• Sinônimo(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
• Fórmula empírica (Notação de Hill): C₂₆H₂₂N₄O₃
• Número CAS: 931706-15-9
• Peso molecular: 438.48
• Código UNSPSC: 12352200
• NACRES: NA.28

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: crystalline solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 5 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: −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
• chave InChI: MNOOVRNGPIWJDI-UHFFFAOYSA-N

Descrição

Descrição geral

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.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable