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Search Results for " aromatase,estrogen "

14

抑制剂 & 化合物

2

天然产物

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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
	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
	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
	Fadrozole is a selective inhibitor of aromatase. It also effective in the treatment of estrogen-dependent diseases including breast cancer.
T71010	Norendoxifen
	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
	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...
T35676	17β-hydroxy Exemestane
	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 = ...
T83907	10-Chloroestra-1,4-diene-3,17-dione 10-chloro-1,4-Estradiene
	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）。

化合物

Fadrozole hydrochloride

Cat.No: T7556

Synonym: CGS 16949A,盐酸法倔唑

Target: Aromatase

Cat.No: T20625

Synonym: 咪鲜胺,Sporgon,Prelude

Target: Estrogen Receptor/ERR, AhR, Androgen Receptor, Antifungal

Cat.No: T4281

Synonym: (E/Z)-N-desmethyl-4-hydroxy Tamoxifen,N-去甲基-4-羟基-,(E/Z)-Endoxifen

Target: Estrogen Receptor/ERR, Aromatase, Estrogen/progestogen Receptor, Parasite, Drug Metabolite

Endoxifen (Z-isomer)

Cat.No: T2280

Synonym: 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

Target: Estrogen Receptor/ERR, EGFR, Potassium Channel, Estrogen/progestogen Receptor, HER

Endoxifen hydrochloride

Cat.No: T6827L

Cat.No: T23549

Target: P450, Aromatase

Cat.No: T11847L

Synonym: R75251 dihydrochloride,利阿唑

Target: P450, Retinoid Receptor

Cat.No: T27868

Synonym: LY-113174,LY113174

Fadrozole HCl hydrate

Cat.No: T7197L

Synonym: Fadrozole,CGS-16949A,Fadrozole hydrochloride hemihydrate,CGS16949A,CGS 16949A

Cat.No: T71010

Liarozole dihydrochloride

Cat.No: T11847

Synonym: R75251 dihydrochloride

Target: Others

Endoxifen mesylate

Cat.No: T71578

17β-hydroxy Exemestane

Cat.No: T35676

10-Chloroestra-1,4-diene-3,17-dione

Cat.No: T83907

Synonym: 10-chloro-1,4-Estradiene

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。

天然产物

Cat.No: T1590

Synonym: CGS 20267,来曲唑

Target: Aromatase, Autophagy

Cat.No: T3390

Target: Apoptosis, Aromatase, p38 MAPK

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