Mefentrifluconazole,1417782-03

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Mefentrifluconazole

CAS No. : 1417782-03-6

MCE 国际站：Mefentrifluconazole

产品活性：Mefentrifluconazole 是一种新型的唑类衍生物，广谱抗真菌 (antifungal agent) 剂。Mefentrifluconazole 是具有强效选择性和口服活性真菌 CYP51 的抑制剂 (K_d= 0.5 nM)，但是对人类芳香化酶 (IC₅₀=0.92 μM) 的抑制活性较小。

研究领域：Anti-infection  |  Metabolic Enzyme/Protease

作用靶点：Fungal  |  Cytochrome P450

In Vivo: Mefentrifluconazole undergoes extensive toxicity testing, including a full program of reproductive toxicity studies. Long term repeated dose toxicity and/or carcinogenicity studies have been conducted in rats, mice, and dogs. In each species, the highest dose level investigated gives rise to systemic toxicity.
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.

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