A CFTR channel inhibitor
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PPQ-102

Item No. 16275

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6,7-dihydro-7,9-dimethyl-6-(5-methyl-2-furanyl)-11-phenyl-pyrimido[4',5':3,4]pyrrolo[1,2-a]quinoxaline-8,10(5H,9)-dione
CAS Number
931706-15-9
Synonyms
  • CFTR Inhibitor IV
  • Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor IV
Molecular Formula
C26H22N4O3
Formula Weight
438.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.2 mg/ml
λmax
211, 329 nm
SMILES
CC1=CC=C(O1)C2C3=C4C(C(N(C)C(N4C)=O)=O)=C(C5=CC=CC=C5)N3C6=C(C=CC=C6)N2
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
InChi Key
MNOOVRNGPIWJDI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    PPQ-102 is a cell-permeable pyrimido-pyrrolo-quinoxalinedione that reversibly inhibits CFTR chloride channels with an IC50 value of 90 nM.1 At 0.5-5 µM, PPQ-102 has been used to reduce the size and number of renal cysts in a neonatal kidney organ culture model of polycystic kidney disease.1 At 1 µM, PPQ-102 can increase vascular endothelial growth factor-A production in cultured airway epithelial NCI-H292 cells, triggering epidermal growth factor receptor phosphorylation.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tradtrantip, L., Sonawane, N.D., Namkung, W., et al. Nanomolar potency pyrimido-pyrrolo-quinoxalinedione CFTR inhibitor reduces cyst size in a polycystic kidney disease model. J. Med. Chem. 52(20), 6447-6455 (2009).

    2. Martin, C., Coolen, N., Wu, Y., et al. CFTR dysfunction induces vascular endothelial growth factor synthesis in airway epithelium. Eur. Respir .J. 42, 1553-1562 (2013).