| Identification | Back Directory | [Name]
PPQ-102 | [CAS]
931706-15-9 | [Synonyms]
CS-1365
PPQ-102
CFTR Inhibitor
PPQ 102, >=98%
PPQ-102, CFTR Inhibitor
CFTR INHIBITOR; PPQ102; PPQ 102
CFTR Inhibitor IV, PPQ-102 - CAS 931706-15-9 - Calbiochem
7,9-Dimethyl-6-(5-methylfuran-2-yl)-11-phenyl-5,6-dihydropyrimido[4',5':3,4]pyrrolo[1,2-a]quin
6,7-Dihydro-7,9-dimethyl-6-(5-methyl-2-furanyl)-11-phenylpyrimido[4',5':3,4]pyrrolo[1,2-a]quinoxaline-8,10(5H,9)-dione
7,9-DIMETHYL-6-(5-METHYL-2-FURYL)-11-PHENYL-6,7-DIHYDROPYRIMIDO[4 ',5':3,4]PYRROLO[1,2-A]QUINOXALINE-8,10(5H,9H)-DIONE
Pyrimido[4',5':3,4]pyrrolo[1,2-a]quinoxaline-8,10(5H,9)-dione, 6,7-dihydro-7,9-dimethyl-6-(5-methyl-2-furanyl)-11-phenyl-
6,7-Dihydro-7,9-dimethyl-6-(5-methyl-2-furanyl)-11-phenylpyrimido[4',5':3,4]pyrrolo[1,2-a]quinoxaline-8,10(5H,9)-dione PPQ-102
PPQ-102 6,7-Dihydro-7,9-dimethyl-6-(5-methyl-2-furanyl)-11-phenylpyrimido[4',5':3,4]pyrrolo[1,2-a]quinoxaline-8,10(5H,9)-dione | [Molecular Formula]
C26H22N4O3 | [MDL Number]
MFCD14824240 | [MOL File]
931706-15-9.mol | [Molecular Weight]
438.48 |
| Chemical Properties | Back Directory | [Melting point ]
>300℃ (ethanol ) | [Boiling point ]
648.7±65.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
-20C | [solubility ]
DMF: 0.2 mg/ml | [form ]
White crystalline solid | [pka]
1.00±0.40(Predicted) | [color ]
Light yellow to yellow | [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 | [InChIKey]
MNOOVRNGPIWJDI-UHFFFAOYSA-N | [SMILES]
[n]21c(c5[n]([c]([n]([c](c5c2c6ccccc6)=O)C)=O)C)C(Nc4c1cccc4)c3[o]c(cc3)C |
| Hazard Information | Back Directory | [Uses]
PPQ-102 (CFTR Inhibitor) is a reversible CFTR inhibitor that completely inhibits CFTR chloride currents (IC50 ~90 nM). PPQ-102 is not affected by membrane potential-dependent cell allocation or blocking efficiency (uncharged at physiological pH) and effectively prevents cyst enlargement in polycystic kidney disease[1]. | [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]
Store at -20°C | [References]
[1] Tradtrantip L, et al. Nanomolar potency pyrimido-pyrrolo-quinoxalinedione CFTR inhibitor reduces cyst size in a polycystic kidney disease model. J Med Chem. 2009 Oct 22;52(20):6447-55. DOI:10.1021/jm9009873 |
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Sigma-Aldrich
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SPIRO PHARMA
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www.spiropharma.com.cn |
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