Androgen Receptor

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研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S2840	Apalutamide (ARN-509)	<1 mg/mL	18 mg/mL	5 mg/mL
S1304	Megestrol Acetate	<1 mg/mL	33 mg/mL	15 mg/mL
S7040	AZD3514	<1 mg/mL	100 mg/mL	100 mg/mL
S4797	Nicergoline	-1 mg/mL	22 mg/mL	-1 mg/mL
S1250	Enzalutamide (MDV3100)	<1 mg/mL	92 mg/mL	<1 mg/mL
S1190	Bicalutamide	<1 mg/mL	86 mg/mL	5 mg/mL
s9045	Triptophenolide	-1 mg/mL	62 mg/mL	-1 mg/mL
S5285	RU58841	<1 mg/mL	73 mg/mL	73 mg/mL
S4836	Nilutamide	<1 mg/mL	63 mg/mL	63 mg/mL
S2803	Galeterone	<1 mg/mL	24 mg/mL	40 mg/mL
S1908	Flutamide	<1 mg/mL	55 mg/mL	55 mg/mL
S2604	Dehydroepiandrosterone (DHEA)	<1 mg/mL	57 mg/mL	57 mg/mL
S2042	Cyproterone Acetate	<1 mg/mL	83 mg/mL	10 mg/mL
S4054	Spironolactone	<1 mg/mL	83 mg/mL	20 mg/mL
S4593	Chlormadinone acetate	<1 mg/mL	27 mg/mL	1 mg/mL
S7559	Darolutamide (ODM-201)	<1 mg/mL	80 mg/mL	38 mg/mL
S7955	EPI-001	<1 mg/mL	79 mg/mL	79 mg/mL
S1140	Andarine	<1 mg/mL	88 mg/mL	88 mg/mL
S4794	Drostanolone Propionate	-1 mg/mL	18 mg/mL	-1 mg/mL
S4795	Trenbolone acetate	-1 mg/mL	62 mg/mL	-1 mg/mL
S2832	Epiandrosterone	<1 mg/mL	29 mg/mL	58 mg/mL
S3946	Mesterolone	-1 mg/mL	13 mg/mL	-1 mg/mL
S3717	Testosterone Enanthate	9 mg/mL	80 mg/mL	80 mg/mL
S4757	Dihydrotestosterone(DHT)	<1 mg/mL	58 mg/mL	58 mg/mL
S1174	Ostarine (GTx-024, MK-2866 )	<1 mg/mL	78 mg/mL	78 mg/mL
S5275	Testolone (RAD140)	-1 mg/mL	78 mg/mL	-1 mg/mL

Androgen Receptor抑制剂（28）
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。	Cancer Cell Int, 2018, 18:71 J Cancer, 2014, 5(2):133-42 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。	Science, 2017, 355(6320):78-83 Science, 2017, 355(6320):84-88 Nat Med, 2018, 24(2):239-246	Survival of mice receiving daily vehicle or MDV3100 treatment and treated with the LHRH-Ant or vehicle (n=10 mice per group). Data combined from two independent experiments.
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。	Cancer Res, 2018, 10.1158/0008-5472.CAN-17-3728 Cancer Res, 2018, 78(13):3659-3671 Int J Cancer, 2012, 131(6):E872-83
s9045^New	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.
S5285^New	RU58841 RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
S4836^New	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。
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。	Biochem Biophys Res Commun, 2016, 477(4):1005-10 Steroids, 2018, 138:82-90	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, 2014, 10.1158/1535-7163.MCT-14-0819 J Biomed Mater Res A, 2016, 104(9):2345-55 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.	Antiviral Res, 2017, 146:76-85 Environ Pollut, 2018, 234:846-854 Leukemia, 2018, 32(1):111-119	(A, B) Indicated HIV-1 latency cells (A. J-LAT 10.6; B. CA5) were treated with levosimendan or spironolactone (5, 10, or 20 μM) in combination with TNFα (10 ng/ml). After 24 hr, mRNA was extracted, and reverse transcribed to cDNA for measurement of HIV-1 initiated or elongated (proximal [Pro], intermediate [Int], and distal [Dis]) transcripts by qPCR. Results were normalized to DMSO control. Values represent the mean ± s.d. (n = 4-6).
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).
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。
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.	Food Addit Contam A, 2013, 30(9):1517-26 J Chromatogr A, 2017, 1490:89-101 J Pharm Biomed Anal, 2018, 158:189-203
S4794^New	Drostanolone Propionate Drostanolone Propionate is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795^New	Trenbolone acetate Trenbolone acetate, a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S3830^New	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.
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。
S3946	Mesterolone Mesterolone is a synthetic steroid with anabolic and androgenic activities.
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。	Drug Test Anal, 2011, 3(5):331-6 J Pharm Biomed Anal, 2013, 84:278-84
S5275^New	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