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PPQ-102 (also known as CFTR Inhibitor) is a potent inhibitor of CFTR (cystic fibrosis transmembrane conductance regulator) discovered from screening of approximately 110000 small synthetic and natural compounds for inhibition of halide influx in CFTR-expressing epithelial cells. PPQ-102 can slow cyst enlargement in polycystic kidney disease and reduce intestinal fluid loss in secretory diarrheas. PPQ-102 completely inhibited CFTR chloride current with an IC50 of approximately 90 nM. Unlike prior CFTR inhibitors, PPQ-102 is uncharged at physiological pH, and therefore not subject to membrane potential-dependent cellular partitioning or block efficiency. Patch-clamp analysis confirmed voltage-independent CFTR inhibition by PPQ-102 and showed stabilization of the channel closed state. PPQ-102 prevented cyst expansion and reduced the size of preformed cysts in a neonatal kidney organ culture model of polycystic kidney disease. PPQ-102 is the most potent CFTR inhibitor identified to date.
| ln Vitro |
In an embryonic kidney organ culture model of Parkinson's disease, PPQ-102 (0, 0.5, 5 μM, 4 days) both prevents and reverses the expansion of renal cysts [1]. Preformed cysts have demonstrated reduced fluid accumulation when exposed to PPQ-102 (0, 0.5, 5 μM, 3 days) [1].
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| ln Vivo |
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: E13.5 embryonic kidneys (embryonic kidney organ culture model of PKD) Tested Concentrations: 0, 0.5, 5 μM Incubation Duration: 3 or 4 days Experimental Results: Remarkably decreased the number and size of renal cysts formed in the 8-Br-cAMP-containing medium (demonstrated ∼60% inhibition of cyst formation at 0.5 μM, near complete absence of cysts at 2.5 and 5 μM). Remarkable decreased cyst size over 1 and 2 days in the 8-Br-cAMP -containing medium. |
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| References |
| Molecular Formula |
C26H22N4O3
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| Molecular Weight |
438.48
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| Exact Mass |
438.169
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| CAS # |
931706-15-9
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| Related CAS # |
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| PubChem CID |
16016583
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
648.7±65.0 °C at 760 mmHg
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| Flash Point |
346.1±34.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.720
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| LogP |
3.48
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
33
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| Complexity |
786
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MNOOVRNGPIWJDI-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
12,14-dimethyl-9-(5-methylfuran-2-yl)-17-phenyl-1,8,12,14-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-2,4,6,10,16-pentaene-13,15-dione
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.70 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2806 mL | 11.4030 mL | 22.8061 mL | |
| 5 mM | 0.4561 mL | 2.2806 mL | 4.5612 mL | |
| 10 mM | 0.2281 mL | 1.1403 mL | 2.2806 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 PPQ-102 prevents and reverses renal cyst expansion in an embryonic kidney organ culture model of PKD.J Med Chem.2009 Oct 22;52(20):6447-55. |
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 Patch-clamp analysis of PPQ-102 inhibition of CFTR.J Med Chem.2009 Oct 22;52(20):6447-55. |
 CFTR inhibition by PPQ-102.
Discovery of pyrimido-pyrrolo-quinoxalinedione (PPQ) CFTR inhibitors.J Med Chem.2009 Oct 22;52(20) |
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