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Anastrozole

CAS No. : 120511-73-1

MCE 國際站：Anastrozole

產品活性：Anastrozole 是一種選擇性的芳香酶 (aromatase) 抑制劑，抑制胎盤芳香化酶，IC₅₀ 為 15 nM。

研究領域：Metabolic Enzyme/Protease

作用靶點：Cytochrome P450

In Vitro: Anastrozole is a comparatively simple, achiral benzyltriazole derivative, that inhibits human placental aromatase with an IC₅₀ of 15 nM. In the same assay it is 200 times as potent as aminoglutethimide (AG), twice as potent as 4-OHA and one third as potent as Fadrozole.

In Vivo: Groups of eight immature (22-day-old) female rats are given androstenedione (AD) (30 mg/kg) in arachis oil s.c. daily for3 days with or without various doses of Anastrozole p.o. on day 4 the uteri are dissected, blotted and weighed. An oral dose of 0.1 mg/kg of Anastrozole given on day 2 or day 3 of the cycle completely blocked ovulation. At the same daily dosage (0.1 mg/kg), Anastrozole completely extinguished the uterotrophic activity of exogenous AD in immature rats. In male pigtailed monkeys, twice-daily oral treatment with 0.1 mg/kg and above of Anastrozole reduced circulating oestradiol concentrations by 50-60%.

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