2. Signaling Pathways
  3. Vitamin D Related/Nuclear Receptor
  4. Androgen Receptor

Androgen Receptor

Androgen Receptor

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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).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-176068
    3-Cl-Pyridine-amide-acrylaldehyde-piperazine
    		99.30%
    3-Cl-Pyridine-amide-acrylaldehyde-piperazine is a synthetic intermediate of LO-4-25 (HY-176067). LO-4-25 is an androgen receptor (AR) DNA binding domain ligand linked via a linker to the truncated fumaramide handle. LO-4-25 shows robust degradation of both AR and AR-V7 in 22Rv1 cells.
    3-Cl-Pyridine-amide-acrylaldehyde-piperazine
  • HY-14650R
    DHEA (Standard)
    		Control
    DHEA (Prasterone) (Standard) is the analytical standard of DHEA. This product is intended for research and analytical applications. DHEA is a steroid hormone.
    DHEA (Standard)
  • HY-16060S1
    Apalutamide-d3
    Apalutamide-d3 is the deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide-d<sub>3</sub>
  • HY-144127
    AR antagonist 3
    		Antagonist 99.96%
    AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally.
    AR antagonist 3
  • HY-N9917
    Galloylalbiflorin
    		Antagonist
    Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgen receptor (AR) antagonist (IC50=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity.
    Galloylalbiflorin
  • HY-70002BS
    Enzalutamide carboxylic acid-d6
    		98.99%
    Enzalutamide carboxylic acid-d6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid). Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide.
    Enzalutamide carboxylic acid-d<sub>6</sub>
  • HY-159639
    BAY-2925976
    		Inhibitor 99.14%
    BAY-2925976 is an α2C adrenergic receptor (ARα2C) antagonist that can be used for the study of obstructive sleep apnea (OSA).
    BAY-2925976
  • HY-163940
    LX1
    		99.13%
    LX1 is an anti-prostate cancer compound that targets androgen receptor (AR), AR variants and steroidogenic enzyme AKR1C3. LX1 inhibits the enzymatic activity of AKR1C3, reduces the conversion of androstenedione to testosterone and reduces the expression of AR and AR-V7 and downregulates their target genes. LX1 overcomes the resistance of tumor cells to Enzalutamide (HY-70002), and the combination with Enzalutamide (HY-70002) further inhibits tumor growth.
    LX1
  • HY-111145
    RD162
    		Antagonist 99.69%
    RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer.
    RD162
  • HY-B0022R
    Flutamide (Standard)
    		Antagonist
    Flutamide (Standard) is the analytical standard of Flutamide. This product is intended for research and analytical applications. Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome.
    Flutamide (Standard)
  • HY-16060S2
    Apalutamide-13C,d3
    		Antagonist 99.90%
    Apalutamide-13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
    Apalutamide-<sup>13</sup>C,d<sub>3</sub>
  • HY-U00229
    Bifluranol
    		Inhibitor 98.88%
    Bifluranol (BX341) is an anti-androgen.
    Bifluranol
  • HY-16985S
    Darolutamide-d4
    		Antagonist
    Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
    Darolutamide-d<sub>4</sub>
  • HY-16985R
    Darolutamide (Standard)
    		Antagonist
    Darolutamide (Standard) is the analytical standard of Darolutamide. This product is intended for research and analytical applications. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.
    Darolutamide (Standard)
  • HY-N2908R
    Atraric acid (Standard)
    		Antagonist
    Atraric acid (Standard) is the analytical standard of Atraric acid. This product is intended for research and analytical applications. Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases[1][2].
    Atraric acid (Standard)
  • HY-115282
    JNJ-63576253 free base
    		Antagonist
    JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC).
    JNJ-63576253 free base
  • HY-159844
    Gridegalutamide
    Gridegalutamide has antiandrogen and antitumor activities.
    Gridegalutamide
  • HY-111421
    ODM-204
    		Inhibitor
    ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.
    ODM-204
  • HY-13702S
    Nilutamide-d6
    		Antagonist 99.77%
    Nilutamide-d6 (Nilandron-d6) is the deuterium labeled Nilutamide. Nilutamide (Nilandron) is a non-steroidal anti-androgen agent proposed in the research of metastatic prostatic carcinoma.
    Nilutamide-d<sub>6</sub>
  • HY-162423
    CYB210010
    		Agonist
    CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2 receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration.
    CYB210010
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity