Fadrozole法倔唑,102676-47-1

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Fadrozole

CAS No. : 102676-47-1

MCE 国际站：Fadrozole

产品活性：Fadrozole (CGS 16949A free base) 是一种有效，选择性和非甾体类的 aromatase 抑制剂，IC₅₀ 值为6.4 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Cytochrome P450

In Vitro: Fadrozole hydrochloride is a very potent inhibitor of both human placental and rat ovarian aromatase. In hamster ovarian slices, fadrozole hydrochloride inhibits the production of estrogen with an IC₅₀ of 0.03 μM. The production of progesterone is inhibited with an IC₅₀ of 120 μM. Synthesis of other cytochrome P-450 dependent steroids can be suppressed to various degrees with higher doses of fadrozole hydrochloride. .

In Vivo: Fadrozole hydrochloride is able to inhibit the aromatase-mediated androstenedione-induced uterine hypertrophy in immature female rats with an ED₅₀ of 0.03 mg/kg when given orally. In the same model, aminoglutethimide elicits the same effect with an ED₅₀ of 30 mg/kg when given orally. Fadrozole hydrochloride prevents the development of both benign and malignant spontaneus mammary neoplasns in female Sprague-Dawley rats. It also slows the spontaneous development of ptuitary pars dta mas in female rats, and reduces the of spontaneous hcu ar tumours in male and female rats. Administration of fadrozole in male and female mice suppresses the production of 17b-estradiol, accompanied with a 70% reduction in parasite burden. This protective effect is associated in male mice with a recovery of the specific cellular immune response. Interleukin-6 (IL-6) serum levels, and its production by splenocytes, is augmented by 80%, together with a 10-fold increase in its expression in testes of infected male mice. Fadrozole treatment returns these levels to baseline values.

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