| Bioactivity | 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]. | ||||||||||||
| Target | IC50: ~90 nM (CFTR). | ||||||||||||
| Invitro | PPQ-102 (0, 0.5, 5μM, 4 days) prevents and reverses renal cyst expansion in an embryonic kidney organ culture model of PKD[1].PPQ-102 (0, 0.5, 5μM, 3 days) shows ability of reducing fluid accumulation in preformed cysts[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| Name | PPQ-102 | ||||||||||||
| CAS | 931706-15-9 | ||||||||||||
| Formula | C26H22N4O3 | ||||||||||||
| Molar Mass | 438.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |