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  3. Aromatase

Aromatase (芳香化酶)

Aromatase (estrogen synthetase, CYP19) is a unique cytochrome P450 that catalyzes the removal of the 19-methyl group and aromatization of the A-ring of androgens for the synthesis of estrogens. All human estrogens are synthesized via this enzymatic aromatization pathway. Aromatase is most widely known for its roles in reproduction and reproductive system diseases, and as a target for inhibitor therapy in estrogen-sensitive diseases including cancer, endometriosis, and leiomyoma.

The selective inhibition of estrogen production by aromatase inhibitors is an efficient strategy for breast cancer treatment. These compounds are classified as irreversible inhibitors of aromatase (type I), and comprise steroidal compounds. Reversible inhibitors of aromatase, which comprises non-steroidal compounds are type II aromatase inhibitors. Second and third generation aromatase inhibitors are considerably more potent and more specific in their ability to inhibit aromatase, as compared with first generation compounds (aminoglutethimide).

Aromatase 相关产品 (14):

目录号 产品名 作用方式 纯度
  • HY-14248
    Letrozole Inhibitor 99.80%
    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 99.99%
    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 ≥98.0%
    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-14247A
    Fadrozole Inhibitor 99.69%
    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。
  • HY-14248S
    Letrozole-d4 Inhibitor
    Letrozole-d4 是 Letrozole 的氘代物。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-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-14247
    Fadrozole hydrochloride Inhibitor 99.22%
    Fadrozole hydrochloride (CGS 16949A) 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-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-N7128
    Flavanone Inhibitor 99.94%
    Flavanone 是一种天然的黄酮类化合物。Flavanone 对人类雌激素合成酶芳香化酶 (aromatase) 具有抑制作用。
  • HY-18719E
    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-N8405
    Isolimonexic acid Inhibitor
    Isolimonexic acid 是从柠檬种子中分离得到的一种类柠檬酸,具有抗癌和抗芳香化酶 (anti-aromatase) (IC50=25.60 μM) 特性。
  • 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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