Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM). Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent.

CYP51A:0.5 nM (kd)

In the acute and repeat dose toxicity studies performed with Mefentrifluconazole.?A single-dose administration to rats the LD50 is >2000?mg/kg bwt by the oral route, >5000?mg/kg bwt by the dermal route, and >5.314?mg/L by inhalation as a dust aerosol.?Mefentrifluconazole is not a skin or an eye irritant, nor is it a phototoxicant in vitro.In the acute neurotoxicity study in rats, Mefentrifluconazole (oral administration;?2000?mg/kg bwt;?single dose) gives rise to reduce body weight gain and transient neurobehavioral effects only on the day of treatment (unsteady gait, reduced motor activity, reduces grip strength of the forelimbs and increased distance between the hind limbs in the landing foot-splay test).In the repeated-dose toxicity studies, the liver is the target organ in each of the three species investigated.?At higher dose levels in the rat (oral diets;?383/334 mg/kg/bwt/d (4000 ppm)) and the C57BL/6JRj mouse (61 mg/kg bwt/d (300 ppm)), reduces body weight gain and food consumption, alters clinical chemistry parameters, increases liver weight and is accompanied by liver cell hypertrophy, and/or liver cell necrosis.?At low doses, increases liver weight is not associated with any histopathological alterations and is considered to be an adaptive change to treatment.