424.08 Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.
Benzbromarone (20 μM) decreases mitochondrial membrane potential by 81%
in isolated rat hepatocytes. Benzbromarone decreases state 3 oxidation
and respiratory control ratios for L-glutamate with IC50
Benzbromarone significantly reduces the oxypurinol uptake at a
concentration as low as 10 nM and completely blocks it at 1 μM.
Benzbromarone (1 μM) uptakes the typical substrate of OCTN1
(tetraethylammonium) and OCTN2 (carnitine) in the HEK293 cells expressed
with human OCTN1 by 96.7% and 111% of control, respectively.
Benzbromarone completely inhibits urate uptake at 50 μM in URAT1-expressing oocytes, with IC50 of less than 0.1 μM. Benzbromarone activates through sequential hydroxylation of the
benzofuran ring to a catechol, which can then be further oxidized to a
reactive quinone intermediate capable of adducting protein.
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