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Aromatase

Aromatase (estrogen synthetase, CYP19) is a member of cytochrome P450 and the only known enzyme catalyzes the biogenesis of estrogens through the aromatization of androgens. For its roles in reproduction system, aromatase is a famous target for inhibitor therapy in estrogen-sensitive diseases including breast cancer, endometriosis, leiomyoma, etc.

Aromatase inhibitors (AIs) are drugs that deplete the levels of estrogens by inhibiting aromatase. AIs can be divided in two types according to their chemical structure, steroidal (Type I) and non-steroidal (type II). AIs can also be grouped in three generations based their chronological order of appearance in clinic. The first-generation AI is aminoglutethimide, the second-generation inhibitors include imidazole, fadrozole and formestane, while the third-generation inhibitors are anastrozole, letrozole, and exemestane.

Aromatase 相关产品 (11):

Cat. No. Product Name Effect Purity
  • HY-14248
    Letrozole Inhibitor 99.92%
    Letrozole (CGS 20267) 是一种有效的,选择性的,可逆的和具有口服活性的非甾体类芳香化酶 (aromatase) 抑制剂,IC50 值为 11.5 nM。Letrozole 选择性抑制雌激素的生物合成,可用于乳腺癌的研究。
  • HY-14274
    Anastrozole Inhibitor 99.93%
    Anastrozole 是一种选择性的芳香酶 (aromatase) 抑制剂,抑制胎盘芳香化酶,IC50 为 15 nM。
  • HY-13632
    Exemestane Inhibitor 99.95%
    Exemestane (FCE 24304) 是一种选择性,不可逆和具有口服活性的甾体芳香酶 (aromatase) 抑制剂,对人胎盘和大鼠卵巢芳香酶的 IC50 分别为 30 nM 和 40 nM。Exemestane 可用于激素依赖性乳腺癌研究。
  • HY-18719B
    Endoxifen hydrochloride 98.32%
    Endoxifen hydrochloride 是Tamoxifen 的关键活性代谢物,与雌激素受体 (estrogen receptor) 有较高的亲和力和特异性,同时也能抑制芳香酶的活性。Endoxifen hydrochloride 有用于乳腺癌研究的潜力。
  • HY-14247
    Fadrozole hydrochloride Inhibitor 99.64%
    Fadrozole hydrochloride 是一种有效,选择性和非甾体类的 aromatase 抑制剂,其 IC50 值为 6.4 nM。
  • HY-14247A
    Fadrozole Inhibitor 99.78%
    Fadrozole是一种有效,选择性和非甾体类的 aromatase 抑制剂,IC50 值为6.4 nM。
  • HY-N0292
    Oleuropein Inhibitor 98.54%
    Oleuropein 在橄榄叶和油中发现的,可通过直接抑制 PPARγ 转录活性来发挥抗氧化,抗炎和抗动脉粥样硬化作用。Oleuropein 通过 p53 依赖性途径以及 BaxBcl2 基因的调控来诱导乳腺癌细胞凋亡。Oleuropein 还抑制芳香化酶 (aromatase)。
  • HY-18719E
    Endoxifen
    Endoxifen 是 Tamoxifen 的关键活性代谢物,与雌激素受体 (estrogen receptor) 有较高的亲和力和特异性,同时也能抑制芳香酶的活性。Endoxifen 有用于乳腺癌研究的潜力。
  • HY-125833
    Alpha-Naphthoflavone Inhibitor 98.02%
    Alpha-Naphthoflavone 是一种合成的黄酮类化合物,为有效、竞争性的芳香酶 aromatase 抑制剂,IC50Ki 值分别为 0.5 和 0.2 μM。
  • HY-136092
    Androsta-1,4,6-triene-3,17-dione Inhibitor
    Androsta-1,4,6-triene-3,17-dione 是亲脂性、特异性的芳香酶 (aromatase) 抑制剂,Ki 值为 0.18 μM。Androsta-1,4,6-triene-3,17-dione 可抑制雌激素生物合成,具有避孕作用。Androsta-1,4,6-triene-3,17-dione 能诱导空间记忆障碍。
  • HY-U00176
    Org30958 Inhibitor
    Org30958 是体内有效的芳香酶 (aromatase) 抑制剂。
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