Androgen Receptor
Androgen receptor (AR) is a type of nuclear receptor that is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. Upon binding the hormone ligand, the receptor dissociates from accessory proteins, translocates into the nucleus, dimerizes, and then stimulates transcription of androgen responsive genes. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression. Androgen regulated genes are critical for the development and maintenance of the male sexual phenotype. Mutations in this gene are also associated with complete androgen insensitivity (CAIS).
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Androgen Receptor Inhibitors
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Androgen Receptor Agonists
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Androgen Receptor Antagonists
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Androgen Receptor Ligands
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Androgen Receptor Related Products (486)
Related Products (486)
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Recombinant Proteins (1)
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Antibodies (2)
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Dibenzyl phthalate
0 ImagesDibenzyl phthalate, a diaryl phthalate, is extensively used as a plasticizer to modify the properties of the synthetic resin substrates, resulting in the improvement of flexibility and durability of the end products. Dibenzyl phthalate is an endocrine-disrupting compound, and activates estrogen and androgen receptors.
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Tibolone-d5
0 ImagesCat. No.: HY-123047STibolone-d5 is deuterium labeled Tibolone. Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
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Chlormadinone (Standard)
0 ImagesCat. No.: HY-135473RCAS No.: 1961-77-9Chlormadinone (Standard) is the analytical standard of Chlormadinone (HY-135473). This product is intended for research and analytical applications. Chlormadinone is an orally active anti-androgen agent. Chlormadinone improves intermittency, terminal dribbling, and urinary stream size and force. Chlormadinone can be used for the research of benign prostatic hyperplasia.
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LGD-2941
0 ImagesCat. No.: HY-111309CAS No.: 847235-85-2LGD-2941 is an orally active, potent and selective androgen receptor modulator. LGD-2941 shows excellent anabolic activity in muscle with reduced effect on the prostate in a rat model of hypogonadism. LGD-2941 also improves bone strength in a rat model of post-menopausal osteoporosis.
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MK-0773 (Standard)
0 ImagesCat. No.: HY-11027RCAS No.: 606101-58-0Synonyms: PF-05314882 (Standard)MK-0773 (Standard) is the analytical standard of MK-0773 (HY-11027). This product is intended for research and analytical applications. MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.
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AR ligand-51
0 ImagesCat. No.: HY-139444CAS No.: 2616553-29-6AR ligand-51 is an androgen receptor ligand, which can be used for the synthesis of PROTACs, such as ARD-2585 (HY-139436).
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p,p'-DDE (Standard)
0 ImagesSynonyms: 4,4'-DDE (Standard); p,p'-Dichlorodiphenyldichloroethylene (Standard)p,p'-DDE (Standard) is the analytical standard of p,p'-DDE. This product is intended for research and analytical applications. p,p'-DDE (4,4'-DDE) is the major and persistent metabolite of DDT. p,p'-DDE is a orally active androgen receptor antagonist with an IC50 of 5 μM and a Ki of 3.5 μM. p,p'-DDE can affect the development and function of the male reproductive system. Additionally, high serum concentrations of p,p'-DDE may be a risk factor for type 2 diabetes in women.
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Apalutamide (Standard)
0 ImagesSynonyms: ARN-509 (Standard)Apalutamide (Standard) is the analytical standard of Apalutamide. This product is intended for research and analytical applications. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
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Bromopropylate
0 ImagesCat. No.: HY-B2044CAS No.: 18181-80-1Bromopropylate is a pesticide with moderate anti-androgenic activities.
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Linuron (Standard)
0 ImagesLinuron (Standard) is the analytical standard of Linuron. This product is intended for research and analytical applications. Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor.
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BMS-986365 (Standard)
0 ImagesCat. No.: HY-158101RCAS No.: 2446928-30-7Synonyms: CC-94676 (Standard)BMS-986365 (Standard) is the analytical standard of BMS-986365 (HY-158101). This product is intended for research and analytical applications. BMS-986365 (CC-94676) is an orally active and selective targeted androgen receptor (AR) PROTAC degrader (DC50 of 10-40 nM). BMS-986365 is capable of inducing cereblon (CRBN) E3 ligase-dependent ubiquitination and degradation of the androgen receptor (AR), as well as various AR mutants. BMS-986365 shows no degradation of the close AR family members estrogen receptor (ER), progesterone receptor (PR), and glucocorticoid receptor (GR). BMS-986365 shows significant in vivo potency, degrading AR, inhibiting AR signaling, and restricting tumor growth in animal models of advanced prostate cancer. BMS-986365 can be used for the study of metastatic castration-resistant prostate cancer (mCRPC).
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ARV-771 (Standard)
0 ImagesCat. No.: HY-100972RCAS No.: 1949837-12-0ARV-771 (Standard) is the analytical standard of ARV-771 (HY-100972). This product is intended for research and analytical applications. ARV-771 is a BET PROTAC degrader, with Kd values of 34, 4.7, 8.3, 7.6, 9.6 and 7.6 nM against BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1) and BRD4 (2) , respectively. ARV-771 inhibits the transcription of AR/AR-v7 and its downstream target genes. By degrading BRD4 protein, ARV-771 enhances the sensitivity of prostate cancer cells to ferroptosis, suppresses cancer cell viability, and induces apoptosis. ARV-771 downregulates the levels of BRD4, c-MYC and AR-V7 in tumor tissues and inhibits tumor tissue growth. ARV-771 can be used in prostate cancer-related research.
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p,p'-DDE-13C12
0 ImagesCat. No.: HY-W753141CAS No.: 201612-50-2Synonyms: 4,4'-DDE-13C12; p,p'-Dichlorodiphenyldichloroethylene-13C12p,p'-DDE-13C12 is 13C labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM.
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Triptophenolide (Standard)
0 ImagesCat. No.: HY-N0475RCAS No.: 74285-86-2Synonyms: Hypolide (Standard); (+)-Triptophenolide (Standard)Triptophenolide (Standard) (Hypolide) is the analytical standard of Triptophenolide (HY-N0475). This product is intended for research and analytical applications. Triptophenolide is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer.
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YK11 (Standard)
0 ImagesCat. No.: HY-107480RCAS No.: 1370003-76-1YK11 (Standard) is the analytical standard of YK11. This product is intended for research and analytical applications. YK11 is a partial agonist of androgen receptor, with osteogenic activity.
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FL442
0 ImagesCat. No.: HY-164477CAS No.: 1431166-12-9FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL).
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Octinoxate-13C,d3
0 ImagesCat. No.: HY-B1234SOctinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.
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Dimethylcurcumin (Standard)
0 ImagesCat. No.: HY-15194RCAS No.: 52328-98-0Synonyms: ASC-J9 (Standard); GO-Y025 (Standard)Dimethylcurcumin (Standard) is the analytical standard of Dimethylcurcumin. This product is intended for research and analytical applications. Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
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Bicalutamide (Standard)
0 ImagesBicalutamide (Standard) is the analytical standard of Bicalutamide. This product is intended for research and analytical applications. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.
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LGD-2226 (Standard)
0 ImagesCat. No.: HY-105318RCAS No.: 328947-93-9LGD-2226 (Standard) is the analytical standard of LGD-2226 (HY-105318). This product is intended for research and analytical applications. LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction.
