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-164371
    (+)-JJ-74-138
    		Antagonist
    (+)-JJ-74-138, a novel non-competitive androgen receptor (AR) antagonist, is capable of inhibiting Enzalutamide-resistant CRPC.
    (+)-JJ-74-138
  • HY-105122
    Zanoterone
    		Antagonist
    Zanoterone is an orally active antagonist of the androgen receptor (AR) with a Ki of 2.2 μM. Zanoterone blocks the binding of androgens such as testosterone and dihydrotestosterone (DHT), inhibiting the androgen signaling pathway, thereby reducing androgen-dependent prostate hyperplasia and prostate cancer growth.
    Zanoterone
  • HY-138089
    17β-Hydroxy exemestane
    		Agonist
    17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.
    17β-Hydroxy exemestane
  • HY-114913
    Fenarimol
    		Inhibitor
    Fenarimol (EL 222) is a potent and orally active fungicide. Fenarimol also is a androgen receptor inhibitor with an IC50 value of 19 µM. Fenarimol decreases the mRNA expression of PBP C3, ODC, IGF-1.
    Fenarimol
  • HY-B0845R
    Prochloraz (Standard)
    		Antagonist
    Prochloraz (Standard) is the analytical standard of Prochloraz. This product is intended for research and analytical applications. Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM.
    Prochloraz (Standard)
  • HY-106104
    Inocoterone acetate
    Inocoterone acetate (RU-38882) is a nonsteroidal antiandrogen. Inocoterone acetate binds to the androgen receptor and has antiandrogenic activity in animal models. Inocoterone acetate reduces inflammatory papules and pustules.
    Inocoterone acetate
  • HY-W653723R
    N-Nitrosodicyclohexylamine (Standard)
    		Antagonist
    N-Nitrosodicyclohexylamine (Standard) is the analytical standard of N-Nitrosodicyclohexylamine. This product is intended for research and analytical applications. N-Nitrosodicyclohexylamine (NDCHA) is a N-nitrosocompound with anti-androgenic activities. N-Nitrosodicyclohexylamine shows the competitive binding to androgen receptor (AR) against 5α-dihydrotestosterone and decreased the level of AR protein.
    N-Nitrosodicyclohexylamine (Standard)
  • HY-135794R
    11-Ketodihydrotestosterone (Standard)
    		Agonist
    11-Ketodihydrotestosterone (Standard) is the analytical standard of 11-Ketodihydrotestosterone. This product is intended for research and analytical applications. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
    11-Ketodihydrotestosterone (Standard)
  • HY-106827S1
    Trimegestone-13C,d3
    		Inhibitor
    Trimegestone-13C,d3 is 13C and deuterated labeled Trimegestone (HY-106827). Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes.
    Trimegestone-<sup>13</sup>C,d<sub>3</sub>
  • HY-114246
    ONC1-13B
    ONC1-13B is a potent androgen receptor (AR) antagonist with the activity of effectively inhibiting PSA expression in prostate cancer cells. ONC1-13B can effectively inhibit PSA expression and prostate cancer cell proliferation under DHT stimulation. ONC1-13B exerts its anti-tumor effect by preventing androgen from binding to AR and its nuclear translocation.
    ONC1-13B
  • HY-W744216
    Trestolone acetate
    		Agonist
    Trestolone acetate is a synthetic anabolic androgenic steroid.
    Trestolone acetate
  • HY-123698
    Mebolazine
    		Agonist
    Mebolazine binds to the androgen receptor and produce androgenic and anabolic activity.
    Mebolazine
  • HY-U00052
    Silandrone
    Silandrone is a synthetic, orally active anabolic-androgenic steroid (AAS).
    Silandrone
  • HY-45509
    TLB 150 Benzoate
    		Modulator
    TLB 150 Benzoate (RAD150) is the modulator for androgen receptor with an IC50 of 0.13 μM.
    TLB 150 Benzoate
  • HY-W653896
    Alternariol-d2
    		Inhibitor
    Alternariol-d2 is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol-d<sub>2</sub>
  • HY-B2044R
    Bromopropylate (Standard)
    		Inhibitor
    Bromopropylate (Standard) is the analytical standard of Bromopropylate. This product is intended for research and analytical applications. Bromopropylate is a pesticide with moderate anti-androgenic activities.
    Bromopropylate (Standard)
  • HY-N6660R
    Trisdecanoin (Standard)
    		Inhibitor
    Trisdecanoin (Standard) is the analytical standard of Trisdecanoin. This product is intended for research and analytical applications. Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics.
    Trisdecanoin (Standard)
  • HY-B1234R
    Octinoxate (Standard)
    		Modulator
    Octinoxate (Standard) is the analytical standard of Octinoxate. This product is intended for research and analytical applications. Octinoxate (Octyl methoxycinnamate) is an organic compound that is an ingredient in some sunscreens and lip balms, primarily used is in sunscreens and other cosmetics to absorb UV-B rays from the sun, protecting the skin from damage and can be used to reduce the appearance of scars. Octinoxate also has a complex androgenic and estrogenic effect.
    Octinoxate (Standard)
  • HY-13604R
    Cyproterone acetate (Standard)
    		Antagonist
    Cyproterone acetate (Standard) is the analytical standard of Cyproterone acetate. This product is intended for research and analytical applications. Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors.
    Cyproterone acetate (Standard)
  • HY-13331S2
    Clascoterone-d5-1
    		Antagonist
    Clascoterone-d5-1 (Cortexolone 17 alpha-propionate-d5-1) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
    Clascoterone-d<sub>5</sub>-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity