Atamestane (SH 489) 是一种特殊的芳香酶抑制剂，可选择性阻断雄烯二酮和睾酮芳香化产生的雌激素生物合成。Atamestane 竞争性且不可逆地抑制雌激素生物合成。Atamestane 可用于良性前列腺增生 (BPH) 的研究。

Atamestane (SH 489) is a specific aromatase inhibitor, which selectively blocks the estrogen biosynthesis resulting from the aromatization of androstenedione and testosterone. Atamestane is a competitive and irreversible inhibitor of estrogen biosynthesis. Atamestane can be used for the research of benign prostatic hyperplasia (BPH) [1].

Atamestane inhibits the growth of Ac-1 cells in vitro with IC 50 value of 60.4±17.2 μM. The combination of Toremifene plus Atamestane is better than Toremifene or Atamestane alone in vitro [2]. Cell Viability Assay [2] Cell Line: Ac-1 cells Concentration: 1, 5, 10, 50, 100, 500, and 1000 μM Incubation Time: 6 days Result: The growth of Ac-1 cells was inhibited by Atamestane in a dose dependent manner with IC 50 value of 60.4±17.2 μM.

Atamestane is a selective, pure, and highly effective steroidal aromatase inhibitor, with an excellent safety profile. Atamestane completely antagonizes all the estrogen-induced changes in the prostate. Atamestane leads to a decrease of pregnant mare serum gonadotropin-stimulated ovarian estrogen production, and inhibits androstenedione-induced estrogenic effects such as uterine growth and abortion in rats. Atamestane inhibits estrogen-related negative feedback. Atamestane is highly effective in inhibiting estrogen-induced hyperplastic changes in the fibromuscular stroma of the prostate in androstenedione-treated dogs and monkeys [1]. Atamestane (1 and 3 mg/animal/day; subcutaneously for 3 days) inhibits ovarian estrogen biosynthesis in pregnant mare serum gonadotropin (PMSG)-primed rats [1]. The combination of Toremifene (1000μg/day) plus Atamestane (1000μg/day) is as effective as Toremifene or Tamoxifen (100μg/day) alone but may not provide any additional benefit over Toremifene alone or Tamoxifen alone in ovariectomized female SCID mice bearing Ac-1 xenografts [2]. Animal Model: Infantile female rats, weighing about 50 g [1] Dosage: 1 and 3 mg/animal/day Administration: Subcutaneously for 3 days Result: Resulted in a significant dose-dependent decrease of the pregnant mare serum gonadotropin (PMSG)-induced, elevated serum estrogen concentration. Animal Model: Ovariectomized female SCID mice bearing Ac-1 xenografts [2] Dosage: Atamestane (1000 μg/day), or the combination of Toremifene (1000 μg/day) plus Atamestane (1000 μg/day) Administration: Injected subcutaneously Result: Caused dose dependent reductions in mean tumor weights. The doses of Toremifene and Atamestane which caused maximum reduction in tumor growth were selected for the combination study.

96301-34-7

C20H26O2

298.42

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years