PF-06807656 is a 3-sulfamoylbenzamide-based renal outer medullary potassium channel (ROMK, CCNJ1, Kir1.1) inhibitor (IC50 = 61 nM by whole cell patch clamp) that is insensitive to K80M or N171D pore mutation and exhibits high selectivity for human over rat species (IC50 against thallium sulfate/TlSO4-stimulated influx = 391 nM vs. >30 μM using human or rat ROMK1-expressing HEK293 cells; 82% vs. 0% inhibition by patch clamp using human or rat ROMK2-expressing HEK293 cells).
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Inhibitors of the renal outer medullary potassium channel (ROMK) show promise as novel mechanism diuretics, with potentially lower risk of diuretic-induced hypokalemia relative to current thiazide and loop diuretics. Here, we report the identification of a novel series of 3-sulfamoylbenzamide
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