Aromatase

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研究领域

抑制剂选择性比较

Aromatase产品

所有产品(9) Aromatase抑制剂(9)

目录号	产品描述	文献引用	实验数据
S1235	Letrozole (CGS 20267) Letrozole (CGS 20267) 是第三代aromatase抑制剂，无细胞试验中IC50为0.07-20 nM。在临床研究中，对17α-OH progesterone、TSH、促黄体激素、促卵泡激素或雄烯二酮的血浆浓度没有作用，不影响正常的尿电解质排泄或甲状腺功能。Letrozole 可诱导自噬。	Horm Behav, 2022, 140:105122 Hum Cell, 2022, 10.1007/s13577-022-00671-y Mol Hum Reprod, 2021, 27(4)gaab013	Uterus from mice treated with Letrozole. (A) 13 weeks old aP2-Cre/ERα^flox/flox mice treated with vehicle have swollen abdomen while littermates treated with Letrozole for 17 days looks normal (B). (C) Uterus from vehicle treated aP2-/ERαflox/flox mice with severe hydrometra. (D) Uterus from Letrozole treated aP2-Cre/ERα^flox/flox mice looks normal.
S1188	Anastrozole (ZD-1033) Anastrozole (ZD-1033) 是第三代非甾体类选择性的aromatase抑制剂。相较于其他aromatase抑制剂，它具有更高的选择性，对内源性内分泌没有影响、对肾上腺类固醇也没有明显作用。	Hum Cell, 2022, 10.1007/s13577-022-00671-y Hum Cell, 2021, 10.1007/s13577-021-00579-z Hum Cell, 2021, 10.1007/s13577-021-00639-4	Cell viability analysis of BCSCs transduced as in A and treated with Anastrozole or Docetaxel, alone or in combination with BKM120 up to 72 hours. Data are mean ± SD of 3 independent experiments.
S1196	Exemestane (FCE 24304) Exemestane (FCE24304, PNU155971) 是一种Aromatase抑制剂，抑制人胎盘和大鼠卵巢芳香化酶，IC50分别为30 nM和40 nM。	Hum Cell, 2022, 10.1007/s13577-022-00671-y Cancers (Basel), 2021, 13(14)3586 Hum Cell, 2021, 10.1007/s13577-021-00639-4	Expression of ER, PR, Bcl-2, HER receptors and CYP19A1 mRNA in MCF-7 and AI-resistant cell lines. (A) Western blot analysis of lysates from MCF-7 cells grown with 10% NCS+10^-7 M testosterone (MCF-7) and LetR-1, LetR-3, ExeR-1 and ExeR-3 grown in their standard growth medium with 10^-6 M letrozole and 10^-7 M exemestane, respectively. β-actin and Hsp70 were used as loading controls. (B) Western blot analysis of lysates from MCF-7, LetR-1 and ExeR-1 cells grown for five days in 10% NCS (C) or 10% NCS + 10^-12 M estradiol (E2), 10% NCS + 10^-7M testosterone (T), 10% NCS + 10^-7 M testosterone + 10^-6 M letrozole (T + L), 10% NCS + 10^-7 M testosterone + 10^-7 M exemestane (T+E). LetR-1 and ExeR-1 cells were withdrawn from testosterone and their respective AI one week before onset of experiment. β-actin was used as loading control. (C) CYP19A1 mRNA level in MCF-7 cells grown with 10% NCS + 10^-7 M testosterone for five days and AI-resistant cell lines grown in their standard medium determined by quantitative RT-PCR
S2208	Formestane Formestane (CGP-32349, NSC 282175)是第二代选择性芳香酶抑制剂，IC50为80 nM。
S1672	Aminoglutethimide Aminoglutethimide (BA-16038, NSC-330915) 是一种芳香化酶抑制剂，IC50为10 μM。	Drug Test Anal, 2020, 10.1002/dta.2917
S9519	Fadrozole (CGS16949A) Fadrozole (CGS16949A)是一种有效的、选择性aromatase抑制剂，IC50为4.5 nM, 对aromatase比对其他细胞色素P450酶更有选择性。	Drug Test Anal, 2020, 10.1002/dta.2917
S5158	alpha-Naphthoflavone Alpha-Naphthoflavone (7,8-benzoflavone), a synthetic flavonoid, is a potent inhibitor of aromatase with an I50 value of 0.5 μM.
S3784	Obacunone (AI3-37934) Obacunone (AI3-37934, CCRIS 8657), a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2.	Cell Mol Biol Lett, 2022, 27(1):29
S7867	Oleuropein Oleuropein 是一种从橄榄叶中分离出的抗氧化多酚。Oleuropein 具有抗氧化、抗炎和抗动脉粥样硬化的作用，并在体外抑制脂肪细胞的分化。Oleuropein 抑制 PPARγ 活性。Oleuropein 通过直接抑制PPARγ转录活性发挥抗脂肪形成作用。Oleuropein 还可抑制aromatase。Oleuropein 可诱导凋亡。Phase 2。	J Med Virol, 2019, 91(8):1440-1447

目录号	产品描述	文献引用	实验数据
S1235	Letrozole (CGS 20267) Letrozole (CGS 20267) 是第三代aromatase抑制剂，无细胞试验中IC50为0.07-20 nM。在临床研究中，对17α-OH progesterone、TSH、促黄体激素、促卵泡激素或雄烯二酮的血浆浓度没有作用，不影响正常的尿电解质排泄或甲状腺功能。Letrozole 可诱导自噬。	Horm Behav,2022, 140:105122 Hum Cell,2022, 10.1007/s13577-022-00671-y Mol Hum Reprod,2021, 27(4)gaab013	Uterus from mice treated with Letrozole. (A) 13 weeks old aP2-Cre/ERα^flox/flox mice treated with vehicle have swollen abdomen while littermates treated with Letrozole for 17 days looks normal (B). (C) Uterus from vehicle treated aP2-/ERαflox/flox mice with severe hydrometra. (D) Uterus from Letrozole treated aP2-Cre/ERα^flox/flox mice looks normal.
S1188	Anastrozole (ZD-1033) Anastrozole (ZD-1033) 是第三代非甾体类选择性的aromatase抑制剂。相较于其他aromatase抑制剂，它具有更高的选择性，对内源性内分泌没有影响、对肾上腺类固醇也没有明显作用。	Hum Cell,2022, 10.1007/s13577-022-00671-y Hum Cell,2021, 10.1007/s13577-021-00579-z Hum Cell,2021, 10.1007/s13577-021-00639-4	Cell viability analysis of BCSCs transduced as in A and treated with Anastrozole or Docetaxel, alone or in combination with BKM120 up to 72 hours. Data are mean ± SD of 3 independent experiments.
S1196	Exemestane (FCE 24304) Exemestane (FCE24304, PNU155971) 是一种Aromatase抑制剂，抑制人胎盘和大鼠卵巢芳香化酶，IC50分别为30 nM和40 nM。	Hum Cell,2022, 10.1007/s13577-022-00671-y Cancers (Basel),2021, 13(14)3586 Hum Cell,2021, 10.1007/s13577-021-00639-4	Expression of ER, PR, Bcl-2, HER receptors and CYP19A1 mRNA in MCF-7 and AI-resistant cell lines. (A) Western blot analysis of lysates from MCF-7 cells grown with 10% NCS+10^-7 M testosterone (MCF-7) and LetR-1, LetR-3, ExeR-1 and ExeR-3 grown in their standard growth medium with 10^-6 M letrozole and 10^-7 M exemestane, respectively. β-actin and Hsp70 were used as loading controls. (B) Western blot analysis of lysates from MCF-7, LetR-1 and ExeR-1 cells grown for five days in 10% NCS (C) or 10% NCS + 10^-12 M estradiol (E2), 10% NCS + 10^-7M testosterone (T), 10% NCS + 10^-7 M testosterone + 10^-6 M letrozole (T + L), 10% NCS + 10^-7 M testosterone + 10^-7 M exemestane (T+E). LetR-1 and ExeR-1 cells were withdrawn from testosterone and their respective AI one week before onset of experiment. β-actin was used as loading control. (C) CYP19A1 mRNA level in MCF-7 cells grown with 10% NCS + 10^-7 M testosterone for five days and AI-resistant cell lines grown in their standard medium determined by quantitative RT-PCR
S2208	Formestane Formestane (CGP-32349, NSC 282175)是第二代选择性芳香酶抑制剂，IC50为80 nM。
S1672	Aminoglutethimide Aminoglutethimide (BA-16038, NSC-330915) 是一种芳香化酶抑制剂，IC50为10 μM。	Drug Test Anal,2020, 10.1002/dta.2917
S9519	Fadrozole (CGS16949A) Fadrozole (CGS16949A)是一种有效的、选择性aromatase抑制剂，IC50为4.5 nM, 对aromatase比对其他细胞色素P450酶更有选择性。	Drug Test Anal,2020, 10.1002/dta.2917
S5158	alpha-Naphthoflavone Alpha-Naphthoflavone (7,8-benzoflavone), a synthetic flavonoid, is a potent inhibitor of aromatase with an I50 value of 0.5 μM.
S3784	Obacunone (AI3-37934) Obacunone (AI3-37934, CCRIS 8657), a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2.	Cell Mol Biol Lett,2022, 27(1):29
S7867	Oleuropein Oleuropein 是一种从橄榄叶中分离出的抗氧化多酚。Oleuropein 具有抗氧化、抗炎和抗动脉粥样硬化的作用，并在体外抑制脂肪细胞的分化。Oleuropein 抑制 PPARγ 活性。Oleuropein 通过直接抑制PPARγ转录活性发挥抗脂肪形成作用。Oleuropein 还可抑制aromatase。Oleuropein 可诱导凋亡。Phase 2。	J Med Virol,2019, 91(8):1440-1447

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