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Endocrinology / Hormones /
Androgen Receptors

Androgen Receptors

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Flutamide

Catalog No. A10402
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Androgen receptor 拮抗剂

Flutamide是一种抗雄激素药物，其活性代谢洛丽塔与Ki值为55nM的雄激素受体结合，可作用于前列腺癌。了解更多

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EPI-001

Catalog No. A15814
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Androgen Receptor 拮抗剂

EPI-001是雄激素受体（AR）的拮抗剂，它通过与AR的N末端结构域（NTD）共价结合并阻断AR及其剪接变体（转录因子IC50）的转录活性所需的蛋白质相互作用抑制AR NTD反式激活6μM）了解更多

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ODM-201

Catalog No. A15797
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Androgen receptor 拮抗剂

ODM-201是一种有效且完全的人类AR（hAR）拮抗剂，IC50值为26 nM。了解更多

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MK-0773

Catalog No. A15164
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Androgen receptor modulator

MK-0773是一种选择性雄激素受体调节剂（SARMs），是一种4-氮杂-类固醇，在人体中表现出组织选择性（IC50 = 6.6 nM）。了解更多

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GSK-2881078

Catalog No. A12645
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androgen receptor modulator

GSK-2881078是一种选择性雄激素受体调节剂（SARM），正在针对肌肉萎缩以改善其身体功能的受试者的肌肉生长和力量进行评估。了解更多

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N-desMethyl EnzalutaMide

Catalog No. A13964
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androgen-receptor (AR) 拮抗剂

N-desMethyl EnzalutaMide用于治疗涉及雄激素，雌激素和孕激素受体的疾病。了解更多

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RU 58841

Catalog No. A11541
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AR 拮抗剂

RU 58841，也称为PSK-3841或HMR-3841，是一种非甾体类抗雄激素药物。了解更多

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Bopindolol malonate

Catalog No. A13398
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Bopindolol malonate是一种非选择性，有效，长效的β肾上腺素受体拮抗剂。它证明了H2O2诱导的脂质过氧化作用的抑制。了解更多

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Megestrol Acetate

Catalog No. A10563
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Megestrol Acetate是具有抗肿瘤特性的孕酮衍生物。了解更多

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AZD3514

Catalog No. A12396
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AR 抑制剂 downregulator

AZD3514是一种有效的雄激素受体下调剂，具有潜在的抗癌活性。了解更多

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BMS564929

Catalog No. A12805
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Androgen receptor (AR) modulator

BMS-564929是一种新型，高效，口服活性，非甾体组织选择性雄激素受体（AR）调节剂，结合到雄激素受体，Ki 为 2.11±0.16 nM。该化合物已被推进临床试验，以治疗与年龄相关的功能衰退。了解更多

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17 alpha-propionate

Catalog No. A10009
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Androgen 拮抗剂

17 alpha-propionate是一种新型的局部和外周选择性雄激素拮抗剂。了解更多

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ASC-J9

Catalog No. A11300
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ASC-J9通过降解全长和剪接变体雄激素受体来抑制去势抵抗性前列腺癌的生长。了解更多

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- Ruibao Chen, .et al. AR Pathway Is Involved in the Regulation of CX43 in Prostate Cancer, Biomed Res Int., 2015, 2015: 514234 PMID: 26491675
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Cyproterone acetate

Catalog No. A11409
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Androgen Receptor 拮抗剂

Cyproterone acetate是17-羟孕酮的合成衍生物，可作为雄激素受体拮抗剂以及具有弱孕激素和糖皮质激素活性的弱孕激素受体激动剂。了解更多

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TOK-001 (Galeterone)

Catalog No. A11138
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CYP17 抑制剂

TOK-001 (Galeterone)既是雄激素受体拮抗剂又是CYP17A1抑制剂。了解更多

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Andarine (GTX-007)

Catalog No. A10076
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Androgen Receptor 激动剂

Andarine (GTX-007)是研究性的选择性雄激素受体调节剂（SARM）。了解更多

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Bicalutamide (Casodex)

Catalog No. A10142
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Androgen Receptor 拮抗剂

Bicalutamide (Casodex)是一种口服非甾体抗雄激素，用于治疗前列腺癌和多毛症。了解更多

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- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Anowara Khatun, .et al. Transcriptional Repression and Protein Degradation of the Ca2+-Activated K+ Channel KCa1.1 by Androgen Receptor Inhibition in Human Breast Cancer Cells, Front Physiol, 2018, 9: 312 PMID: 29713287
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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(R)-Bicalutamide

Catalog No. A10008
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Androgen Receptor 拮抗剂

(R)-Bicalutamide是一种活性的竞争性非甾体雄激素受体拮抗剂，对MDA 453细胞的IC50为0.17μM。了解更多

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MDV3100

Catalog No. A10562
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Androgen receptor 拮抗剂

MDV3100(Enzalutamide)是一种androgen-receptor (AR)拮抗剂。在AR研究中强烈推荐的抑制剂。了解更多

Product Citations (3)

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- Shiv Verma, .et al. Increased cytokine gene expression and cognition risk associated with androgen deprivation therapy, Prostate, 2022, Oct;82(14):1389-1399 PMID: 35821621
- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Prem P Kushwaha, .et al. Role of solute carrier transporters SLC25A17 and SLC27A6 in acquired resistance to enzalutamide in castration-resistant prostate cancer, Mol Carcinog, 2021, Dec 22 PMID: 34939235
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Ostarine (MK-2866, GTx-024)

Catalog No. A10253
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Androgen Receptor Modulators

Ostarine (MK-2866,GTX-024)是一种雄激素受体调节剂(SARM)。了解更多

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