Androgen Receptor

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研究领域

抑制剂选择性比较

Androgen Receptor产品

所有产品 Androgen Receptor抑制剂(4) Androgen Receptor拮抗剂(14) Androgen Receptor激动剂(11) Androgen Receptor调节剂(3) 新Androgen Receptor产品

产品目录	产品描述	文献引用	实验数据
S2840	Apalutamide (ARN-509) Apalutamide (ARN-509)是一种选择性的，竞争性androgen receptor抑制剂，无细胞试验中IC50为16 nM，对前列腺癌的治疗有效。Phase 3。	Int J Cancer, 2019, 145(5):1382-1394 Cancer Cell Int, 2018, 18:71 Clin Cancer Res, 2017, 23(24):7608-7620	ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).
S1304	Megestrol Acetate Megestrol Acetate是一种人工合成的孕酮，抑制HegG2，IC50为260μM。	Onco Targets Ther, 2017, 10:4809-4819 Sci Rep, 2017, 7(1):12754	HEC-1A cells were treated with pterostilbene (75 μM), megestrol acetate (75 μM) or the combination for 24 h. Whole cell lysates were collected and measured for the change of cell cycle and apoptosis pathways by Western blot. Results are representative of 3 or more preparations.
S7040	AZD3514 AZD3514是一种口服的有效androgen receptor（雄激素受体）抑制剂，K_i为2.2 μM，且降低AR蛋白表达。Phase 1。
S4797	Nicergoline Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has a selective alpha-1A adrenergic receptor blocking property and also other additional mechanisms of actions.
S1250	Enzalutamide (MDV3100) Enzalutamide (MDV3100)是一种androgen-receptor (AR)拮抗剂，在 LNCaP细胞中IC50为36 nM。	Cancer Discov, 2019, 10.1158/2159-8290 Cancer Cell, 2019, 35(3):385-400 J Clin Invest, 2019, 129(2):569-582
S1190	Bicalutamide Bicalutamide是一种androgen receptor (AR)拮抗剂，在LNCaP/AR(cs)细胞系中IC50为0.16 μM。	Int J Cancer, 2019, 145(5):1382-1394 J Exp Clin Cancer Res, 2019, 38(1):337 Mol Cancer Res, 2019, 17(5):1166-1179	Immunohistochemical staining of Ki67 was performed to determine cell proliferation in the tumors. Each tissue section was counted manually in three different areas to assess the Ki67-positive cell index. Data were then presented as number of Ki67-positive cells per x 400 microscope field. Results are presented as the means s.d. **P < 0.001 by Student 's t-test, compared with control.
S2803	Galeterone Galeterone是一种选择性CYP17抑制剂，也是androgen receptor (AR)（雄激素受体）拮抗剂，IC50分别为300 nM和384 nM，也有效抑制人类前列腺肿瘤生长。Phase 2。	Steroids, 2018, 138:82-90 Biochem Biophys Res Commun, 2016, 477(4):1005-10	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S1908	Flutamide Flutamide是一种抗雄激素药物，与雄激素受体有结合活性，K_i为55 nM，主要用于治疗前列腺癌。	Mol Cancer Ther, 2018, 17(10):2091-2099 Environ Pollut, 2018, 234:846-854 J Appl Toxicol, 2017, 37(8):933-942	Active Stat5a/b increases nuclear levels of antiandrogen-liganded AR in PC-3 cells. PC-3 cells were infected with AdAR, AdPrlR and AdWTStat5a, serum-starved for 12 h, and pretreated with 1 nM DHT, 10 μM Bicalutamide (Bic), 10 μM Flutamide (Flu) or 10 μM MDV3100 (MDV) for 1 h before stimulation with 10 nM Prl for 30 min, where indicated. Immunostaining depicts DAPI, Stat5a/b, AR and merged imaging of Stat5a/b and AR.
S2604	Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone (DHEA)是一种重要的内源性类固醇激素，作为androgen receptor拮抗剂以及 estrogen receptor 激动剂。	Cancer Lett, , 382(2):195-202
S2042	Cyproterone Acetate Cyproterone Acetate是雄激素受体拮抗剂，IC50为7.1 nM，也是微弱的孕激素受体激动剂，具有微弱的孕激素和糖皮质激素活性。	Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332	(C) Effect of AR antagonist cyproterone acetate (0–5 nM) on androgen-induced ADTRP transactivation in HeLa cells. (D) Effect of AR antagonist cyproterone acetate (0–0.5 nM) on androgen-induced ADTRP transactivation in HeLa cells
S4054	Spironolactone Spironolactone是一种强有效的雄激素受体拮抗剂， IC50为77 nM.	Environ Pollut, 2018, 234:846-854 Leukemia, 2018, 32(1):111-119 Antiviral Res, 2017, 146:76-85	(h and i) Triptolide inhibits transcription. After exposure to triptolide (1 μm), spironolactone (10 μm), actinomycin D (2 μm, transcription inhibitor used as a positive control) or DMSO for 6 h, the global RNA synthesis was evaluated by the measurement of 5-EU incorporation. The figure shows representative merged pictures of DAPI and 5-EU signal. The intensity of the signal was evaluated through fluorescence microscopy (h) and quantified with the CellProfiler Software. Triptolide but not spironolactone inhibits global transcription.
S4836	Nilutamide Nilutamide是一种非甾体类抗雄性激素药物，对androgen receptors具有亲和力。用于治疗前列腺癌。
S4593	Chlormadinone acetate Chlormadinone acetate是一种甾族的黄体酮，具有抗雄激素和抗促性腺激素的作用。其半衰期约为34-38小时。
S7559	Darolutamide (ODM-201) Darolutamide (ODM-201)是一种新型androgen receptor (AR)拮抗剂，能够阻断AR核转运，其K_i为f 11 nM。Phase 3。	Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1469	Growth suppression effect of different antiandrogens and Chk1 inhibitors on MDA-MB-453 and SUM185PE cells. The effects of a range of concentrations of three antiandrogens (enzalutamide, ENZA; darolutamide, ODM-201; and abiraterone acetate, AA) and two Chk1 inhibitors (GDC-0575 and AZD7762) were assessed by MTT. Histograms represent the respective IC50s (mean of n = 3–4 experiments; error bars show the 95% confidence interval).
S5285	RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
S7955	EPI-001 EPI-001是androgen receptor N-端结构域的拮抗剂，也是一种选择性PPAR-gamma调节剂。	Prostate, 2019, 79(2):206-214
s9045	Triptophenolide Triptophenolide, derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.
S5023	Nadolol Nadolol是一种非选择性的β-肾上腺素能受体拮抗剂，具有抗高血压和抗心律失常活性。
S1140	Andarine Andarine是一种选择性的非甾体类androgen receptor (AR)（雄激素受体）激动剂，K_i为4 nM，对合成代谢器官具有组织选择性。Phase 3.	J Pharm Biomed Anal, 2018, 158:189-203 J Chromatogr A, 2017, 1490:89-101 Food Addit Contam A, 2013, 30(9):1517-26
S6407^New	Tulobuterol hydrochloride Tulobuterol是长效的β2-adrenergic receptor激动剂，具有支气管扩张、消炎和抗病毒活性。
S6352^New	Androsterone Androsterone是源于性激素的类固醇代谢产物，具有较弱的雄激素属性。
S2832	Epiandrosterone Epiandrosterone是一种类固醇激素，具有微弱的雄激素活性，是DHEA的一种天然代谢产物。
S3830	Protodioscin Protodioscin, a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
S3946	Mesterolone Mesterolone is a synthetic steroid with anabolic and androgenic activities.
S4794	Drostanolone Propionate Drostanolone Propionate is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795	Trenbolone acetate Trenbolone acetate, a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S3717	Testosterone Enanthate Testosterone Enanthate是一种雄激素和合成代谢类固醇，用于治疗雄性素补疗。
S3715	Boldenone Undecylenate Boldenone是androgen receptor (AR)的激动剂。Boldenone Undecylenate是睾酮的衍生物，具有强效合成作用，但仅具有中等适度的雄激素活性。
S4757	Dihydrotestosterone(DHT) Dihydrotestosterone是一种内源性的雄激素性类固醇和激素，是雄激素受体的激动剂，其亲和力比睾酮高2-3倍，诱导雄激素受体信号的效力比睾酮高3倍。
S1174	Ostarine (GTx-024, MK-2866 ) MK-2866 (GTx-024)是一种selective androgen receptor modulator (SARM)（选择性雄激素受体调节剂）， K_i为3.8 nM，作用于合成代谢器官具有组织选择性。Phase 3。	J Pharm Biomed Anal, 2013, 84:278-84 Drug Test Anal, 2011, 3(5):331-6
S8822^New	Ligandrol (LGD-4033, VK-5211) Ligandrol (LGD-4033, VK-5211)是一种新型非类固醇的、具有口服选择性的androgen receptor调节剂，对雄激素受体具有高亲和力（Kd约为1 nM）和高选择性。
S5275	Testolone (RAD140) RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.

产品目录	产品描述	文献引用	实验数据
S2840	Apalutamide (ARN-509) Apalutamide (ARN-509)是一种选择性的，竞争性androgen receptor抑制剂，无细胞试验中IC50为16 nM，对前列腺癌的治疗有效。Phase 3。	Int J Cancer,2019, 145(5):1382-1394 Cancer Cell Int,2018, 18:71 Clin Cancer Res,2017, 23(24):7608-7620	ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).
S1304	Megestrol Acetate Megestrol Acetate是一种人工合成的孕酮，抑制HegG2，IC50为260μM。	Onco Targets Ther,2017, 10:4809-4819 Sci Rep,2017, 7(1):12754	HEC-1A cells were treated with pterostilbene (75 μM), megestrol acetate (75 μM) or the combination for 24 h. Whole cell lysates were collected and measured for the change of cell cycle and apoptosis pathways by Western blot. Results are representative of 3 or more preparations.
S7040	AZD3514 AZD3514是一种口服的有效androgen receptor（雄激素受体）抑制剂，K_i为2.2 μM，且降低AR蛋白表达。Phase 1。
S4797	Nicergoline Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has a selective alpha-1A adrenergic receptor blocking property and also other additional mechanisms of actions.

产品目录	产品描述	文献引用	实验数据
S1250	Enzalutamide (MDV3100) Enzalutamide (MDV3100)是一种androgen-receptor (AR)拮抗剂，在 LNCaP细胞中IC50为36 nM。	Cancer Discov, 2019, 10.1158/2159-8290 Cancer Cell, 2019, 35(3):385-400 J Clin Invest, 2019, 129(2):569-582
S1190	Bicalutamide Bicalutamide是一种androgen receptor (AR)拮抗剂，在LNCaP/AR(cs)细胞系中IC50为0.16 μM。	Int J Cancer, 2019, 145(5):1382-1394 J Exp Clin Cancer Res, 2019, 38(1):337 Mol Cancer Res, 2019, 17(5):1166-1179	Immunohistochemical staining of Ki67 was performed to determine cell proliferation in the tumors. Each tissue section was counted manually in three different areas to assess the Ki67-positive cell index. Data were then presented as number of Ki67-positive cells per x 400 microscope field. Results are presented as the means s.d. **P < 0.001 by Student 's t-test, compared with control.
S2803	Galeterone Galeterone是一种选择性CYP17抑制剂，也是androgen receptor (AR)（雄激素受体）拮抗剂，IC50分别为300 nM和384 nM，也有效抑制人类前列腺肿瘤生长。Phase 2。	Steroids, 2018, 138:82-90 Biochem Biophys Res Commun, 2016, 477(4):1005-10	C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05.
S1908	Flutamide Flutamide是一种抗雄激素药物，与雄激素受体有结合活性，K_i为55 nM，主要用于治疗前列腺癌。	Mol Cancer Ther, 2018, 17(10):2091-2099 Environ Pollut, 2018, 234:846-854 J Appl Toxicol, 2017, 37(8):933-942	Active Stat5a/b increases nuclear levels of antiandrogen-liganded AR in PC-3 cells. PC-3 cells were infected with AdAR, AdPrlR and AdWTStat5a, serum-starved for 12 h, and pretreated with 1 nM DHT, 10 μM Bicalutamide (Bic), 10 μM Flutamide (Flu) or 10 μM MDV3100 (MDV) for 1 h before stimulation with 10 nM Prl for 30 min, where indicated. Immunostaining depicts DAPI, Stat5a/b, AR and merged imaging of Stat5a/b and AR.
S2604	Dehydroepiandrosterone (DHEA) Dehydroepiandrosterone (DHEA)是一种重要的内源性类固醇激素，作为androgen receptor拮抗剂以及 estrogen receptor 激动剂。	Cancer Lett, , 382(2):195-202
S2042	Cyproterone Acetate Cyproterone Acetate是雄激素受体拮抗剂，IC50为7.1 nM，也是微弱的孕激素受体激动剂，具有微弱的孕激素和糖皮质激素活性。	Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332	(C) Effect of AR antagonist cyproterone acetate (0–5 nM) on androgen-induced ADTRP transactivation in HeLa cells. (D) Effect of AR antagonist cyproterone acetate (0–0.5 nM) on androgen-induced ADTRP transactivation in HeLa cells
S4054	Spironolactone Spironolactone是一种强有效的雄激素受体拮抗剂， IC50为77 nM.	Environ Pollut, 2018, 234:846-854 Leukemia, 2018, 32(1):111-119 Antiviral Res, 2017, 146:76-85	(h and i) Triptolide inhibits transcription. After exposure to triptolide (1 μm), spironolactone (10 μm), actinomycin D (2 μm, transcription inhibitor used as a positive control) or DMSO for 6 h, the global RNA synthesis was evaluated by the measurement of 5-EU incorporation. The figure shows representative merged pictures of DAPI and 5-EU signal. The intensity of the signal was evaluated through fluorescence microscopy (h) and quantified with the CellProfiler Software. Triptolide but not spironolactone inhibits global transcription.
S4836	Nilutamide Nilutamide是一种非甾体类抗雄性激素药物，对androgen receptors具有亲和力。用于治疗前列腺癌。
S4593	Chlormadinone acetate Chlormadinone acetate是一种甾族的黄体酮，具有抗雄激素和抗促性腺激素的作用。其半衰期约为34-38小时。
S7559	Darolutamide (ODM-201) Darolutamide (ODM-201)是一种新型androgen receptor (AR)拮抗剂，能够阻断AR核转运，其K_i为f 11 nM。Phase 3。	Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1469	Growth suppression effect of different antiandrogens and Chk1 inhibitors on MDA-MB-453 and SUM185PE cells. The effects of a range of concentrations of three antiandrogens (enzalutamide, ENZA; darolutamide, ODM-201; and abiraterone acetate, AA) and two Chk1 inhibitors (GDC-0575 and AZD7762) were assessed by MTT. Histograms represent the respective IC50s (mean of n = 3–4 experiments; error bars show the 95% confidence interval).
S5285	RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
S7955	EPI-001 EPI-001是androgen receptor N-端结构域的拮抗剂，也是一种选择性PPAR-gamma调节剂。	Prostate, 2019, 79(2):206-214
s9045	Triptophenolide Triptophenolide, derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.
S5023	Nadolol Nadolol是一种非选择性的β-肾上腺素能受体拮抗剂，具有抗高血压和抗心律失常活性。

产品目录	产品描述	文献引用
S1140	Andarine Andarine是一种选择性的非甾体类androgen receptor (AR)（雄激素受体）激动剂，K_i为4 nM，对合成代谢器官具有组织选择性。Phase 3.	J Pharm Biomed Anal, 2018, 158:189-203 J Chromatogr A, 2017, 1490:89-101 Food Addit Contam A, 2013, 30(9):1517-26
S6407^New	Tulobuterol hydrochloride Tulobuterol是长效的β2-adrenergic receptor激动剂，具有支气管扩张、消炎和抗病毒活性。
S6352^New	Androsterone Androsterone是源于性激素的类固醇代谢产物，具有较弱的雄激素属性。
S2832	Epiandrosterone Epiandrosterone是一种类固醇激素，具有微弱的雄激素活性，是DHEA的一种天然代谢产物。
S3830	Protodioscin Protodioscin, a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
S3946	Mesterolone Mesterolone is a synthetic steroid with anabolic and androgenic activities.
S4794	Drostanolone Propionate Drostanolone Propionate is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795	Trenbolone acetate Trenbolone acetate, a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S3717	Testosterone Enanthate Testosterone Enanthate是一种雄激素和合成代谢类固醇，用于治疗雄性素补疗。
S3715	Boldenone Undecylenate Boldenone是androgen receptor (AR)的激动剂。Boldenone Undecylenate是睾酮的衍生物，具有强效合成作用，但仅具有中等适度的雄激素活性。
S4757	Dihydrotestosterone(DHT) Dihydrotestosterone是一种内源性的雄激素性类固醇和激素，是雄激素受体的激动剂，其亲和力比睾酮高2-3倍，诱导雄激素受体信号的效力比睾酮高3倍。

产品目录	产品描述	文献引用
S1174	Ostarine (GTx-024, MK-2866 ) MK-2866 (GTx-024)是一种selective androgen receptor modulator (SARM)（选择性雄激素受体调节剂）， K_i为3.8 nM，作用于合成代谢器官具有组织选择性。Phase 3。	J Pharm Biomed Anal, 2013, 84:278-84 Drug Test Anal, 2011, 3(5):331-6
S8822^New	Ligandrol (LGD-4033, VK-5211) Ligandrol (LGD-4033, VK-5211)是一种新型非类固醇的、具有口服选择性的androgen receptor调节剂，对雄激素受体具有高亲和力（Kd约为1 nM）和高选择性。
S5275	Testolone (RAD140) RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.

产品目录

产品描述

文献引用

实验数据

S1174

Ostarine (GTx-024, MK-2866 )

MK-2866 (GTx-024)是一种selective androgen receptor modulator (SARM)（选择性雄激素受体调节剂） ， K_i为3.8 nM，作用于合成代谢器官具有组织选择性。Phase 3。

J Pharm Biomed Anal, 2013, 84:278-84

Drug Test Anal, 2011, 3(5):331-6

S8822^New

Ligandrol (LGD-4033, VK-5211)

Ligandrol (LGD-4033, VK-5211)是一种新型非类固醇的、具有口服选择性的androgen receptor调节剂，对雄激素受体具有高亲和力（Kd约为1 nM）和高选择性。

S5275

Testolone (RAD140)

RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.

研究领域

产品类型

Androgen Receptor

信号通路图

研究领域

抑制剂选择性比较

Androgen Receptor产品