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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7556 |
Fadrozole hydrochloride
CGS 16949A,盐酸法倔唑 |
Aromatase | Endocrinology/Hormones |
Fadrozole hydrochloride (CGS 16949A) 是一种选择性的、有效,和非甾体类的芳香化酶抑制剂(IC50:6.4 nM)。 | |||
T20625 |
Prochloraz
咪鲜胺,Sporgon,Prelude |
Estrogen Receptor/ERR; AhR; Androgen Receptor; Antifungal | Endocrinology/Hormones; Immunology/Inflammation; Metabolism; Microbiology/Virology |
Prochloraz (Prelude) 是咪唑类抗真菌剂。Prochloraz 抑制羊毛甾醇的细胞色素 P450 依赖性 14α-脱甲基作用,由此抑制麦角固醇的生物合成,从而导致真菌细胞膜破裂和细胞死亡。它也是雌激素受体和 雄激素受体的拮抗剂,IC50分别为25 μM 和4 μM, 并激活芳烃受体,EC50为1μM。 | |||
T4281 |
Endoxifen
(E/Z)-N-desmethyl-4-hydroxy Tamoxifen,N-去甲基-4-羟基-,(E/Z)-Endoxifen |
Estrogen Receptor/ERR; Aromatase; Estrogen/progestogen Receptor; Parasite; Drug Metabolite | Endocrinology/Hormones; Metabolism; Microbiology/Virology |
Endoxifen ((E/Z)-Endoxifen) 是 Tamoxifen 的关键活性代谢物,能抑制芳香酶的活性,与雌激素受体有较高的亲和力和特异性。它有潜力研究乳腺癌。 | |||
T2280 |
Endoxifen (Z-isomer)
Z-因多昔芬,Endoxifen Z-isomer,4-[(1E)-1-{4-[2-(甲基氨基)乙氧基]苯基}-2-苯基-1-丁烯-1-基]苯酚 |
Estrogen Receptor/ERR; EGFR; Potassium Channel; Estrogen/progestogen Receptor; HER | Angiogenesis; Endocrinology/Hormones; JAK/STAT signaling; Membrane transporter/Ion channel; Tyrosine Kinase/Adaptors |
Endoxifen Z-isomer (EDX)是 Tamoxifen 重要的代谢产物,在表达 ERα的乳腺癌细胞中发挥抗雌激素作用。它以浓度依赖的方式抑制 hERG, IC50值为1.6μM。 | |||
T6827L |
Endoxifen hydrochloride
|
Others | Others |
Endoxifen hydrochloride,Tamoxifen的主要活性代谢产物,具备较高的对雌激素受体(estrogen receptor)的亲和力和特异性,并能抑制芳香酶活性。它在乳腺癌研究中表现出潜在应用价值。 | |||
T23549 |
YM 511
|
P450; Aromatase | Endocrinology/Hormones; Metabolism |
YM 511 是一种高度特异性的非甾体芳香酶 (aromatase) 抑制剂。YM 511 竞争性抑制大鼠卵巢和人胎盘微粒体中的芳香酶活性 (IC50 分别为 0.4 和 0.12 nM)。YM 511 轻微抑制其他类固醇激素的产生。YM 511 具有用于抑制雌激素依赖性作用研究,不会影响其他类固醇激素的血清水平的潜力。 | |||
T11847L |
Liarozole
R75251 dihydrochloride,利阿唑 |
P450; Retinoid Receptor | Metabolism |
Liarozole (R75251 dihydrochloride) 是一种咪唑衍生物,是一种具有口服活性的维甲酸 (RA) 代谢阻断剂(RAMBA),具有抗肿瘤作用。它能够抑制维甲酸依赖的细胞色素P450(CYP26) 4- 羟基化 (IC50=7 μM),导致组织维甲酸水平增加。 | |||
T27868 |
LY 113174
LY-113174,LY113174 |
Others | Others |
LY 113174, a novel nonsteroidal aromatase inhibitor, may prove useful in the treatment of estrogen-dependent diseases. | |||
T7197L |
Fadrozole HCl hydrate
Fadrozole,CGS-16949A,Fadrozole hydrochloride hemihydrate,CGS16949A,CGS 16949A |
Others | Others |
Fadrozole is a selective inhibitor of aromatase. It also effective in the treatment of estrogen-dependent diseases including breast cancer. | |||
T71010 |
Norendoxifen
|
Others | Others |
Norendoxifen, also known as 4-hydroxy-N, N-didesmethyltamoxifen, is a nonsteroidal aromatase inhibitor of the triphenylethylene group that was never marketed. It is an active metabolite of the selective estrogen receptor modulator tamoxifen. | |||
T11847 |
Liarozole dihydrochloride
R75251 dihydrochloride |
Others | Others |
Liarozole dihydrochloride is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders. | |||
T71578 |
Endoxifen mesylate
|
Others | Others |
Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is a chemical that is under development for estrogen receptor-positive breast cancer. It is also being evaluated as an antipsychotic for treatment of mania and other psychotic disorders. Endoxifen is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group. It is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromat... | |||
T83907 |
10-Chloroestra-1,4-diene-3,17-dione
10-chloro-1,4-Estradiene |
Others | Others |
10-Chloroestra-1,4-diene-3,17-dione 是一个对雌性激素受体α (ERα) 具有激动作用的类固醇。它能增加在S. cerevisiae 中报告基因的表达(对人类受体的EC50 = 0.36 nM)。同时,它也是一种芳香化酶抑制剂(IC50 = 2.4 µM)。 | |||
T35676 |
17β-hydroxy Exemestane
|
Others | Others |
17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = ... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1590 |
Letrozole
CGS 20267,来曲唑 |
Aromatase; Autophagy | Autophagy; Endocrinology/Hormones |
Letrozole (CGS 20267) 是一种可口服的,选择性可逆的非甾体类芳香化酶抑制剂,IC50值为 11.5 nM。它选择性抑制雌激素的生物合成,可研究乳腺癌。 | |||
T3390 |
Obacunone
|
Apoptosis; Aromatase; p38 MAPK | Apoptosis; Endocrinology/Hormones; MAPK |
Obacunone 是从沼泽白葡萄柚种子中分离得到的,通过诱导凋亡发挥抗癌作用。它在雄激素依赖性人前列腺 Y 细胞中具有细胞毒性。它对鼠伤寒沙门氏菌具有抗毒作用,可作为开发鼠伤寒沙门氏菌抗毒策略的先导化合物。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-00956 |
Aromatase/CYP19A1 Protein, Human, Recombinant (His)
ARO1,CYP19A1,Estrogen synthase,Cytochrome P450 19A1... |
Human | E. coli |
Aromatase/CYP19A1 Protein, Human, Recombinant (His) is expressed in E. coli. |