PPQ-102 (Synonyms: CFTR Inhibitor IV, Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor IV) |
| カタログ番号GC17616 |
PPQ-102 (CFTR Inhibitor) は可逆的な CFTR 阻害剤で、CFTR 塩化物電流を完全に阻害します (IC50 ~90 nM)。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 931706-15-9
Sample solution is provided at 25 µL, 10mM.
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PPQ-102 is a potent CFTR inhibitor which can completely inhibited CFTR chloride current with IC50 of ~90 nM. IC50 value: 90 nM [1]Target: CFTRin vitro: The most potent compound, 7,9-dimethyl-11-phenyl-6-(5-methylfuran-2-yl)-5,6-dihydro-pyrimido[4',5'-3,4]pyrrolo[1,2-a]quinoxaline-8,10-(7H,9H)-dione, PPQ-102, completely inhibited CFTR chloride current with IC(50) approximately 90 nM. The PPQs, unlike prior CFTR inhibitors, are 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 [1]. The three gpSlc26 anion transporters exhibited distinct pharmacological profiles of (36)Cl(-) influx, including partial sensitivity to CFTR inhibitors Inh-172 and GlyH101, but only Slc26a11 was inhibited by PPQ-102 [2]. Airway epithelial NCI-H292 cells and primary cultures of noncystic fibrosis human airway epithelial cells were treated with cystic fibrosis transmembrane conductance regulator (CFTR) inhibitors (CFTR-inh(172) or PPQ-102) or transfected with a CFTR small interfering (si)RNA with or without a selective epidermal growth factor receptor tyrosine kinase inhibitor [3].in vivo: 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 [1].
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.
[2]. Stewart AK, et al. SLC26 anion exchangers of guinea pig pancreatic duct: molecular cloning and functional characterization. Am J Physiol Cell Physiol. 2011 Aug;301(2):C289-303.
[3]. Martin C, et al. CFTR dysfunction induces vascular endothelial growth factor synthesis in airway epithelium. Eur Respir J. 2013 Dec;42(6):1553-62.
| Cas No. | 931706-15-9 | SDF | |
| 同義語 | CFTR Inhibitor IV, Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor IV | ||
| Chemical Name | 7,9-dimethyl-6-(5-methylfuran-2-yl)-11-phenyl-5,6-dihydropyrimido[4',5':3,4]pyrrolo[1,2-a]quinoxaline-8,10(7H,9H)-dione | ||
| Canonical SMILES | CC(O1)=CC=C1C(NC2=CC=CC=C2N34)C4=C(N(C5=O)C)C(C(N5C)=O)=C3C6=CC=CC=C6 | ||
| Formula | C26H22N4O3 | M.Wt | 438.48 |
| 溶解度 | DMF: 0.2 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2806 mL | 11.403 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 |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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