Androgen Receptors

Androgen receptors (ARs) (dihydrotestosterone receptors) are nuclear hormone receptors of the NR3C class, which includes mineralocorticoid, progesterone and glucocorticoid receptors. ARs are expressed in bone marrow, mammary gland and prostate tissues.

Products
Background
Gene Data

Androgen Receptor Agonists

Cat. No. Product Name / Activity
5274 BMS 564929
Highly potent and muscle-selective androgen receptor (AR) agonist
3812 Cl-4AS-1
Steroidal androgen receptor agonist

Androgen Receptor Antagonists

Cat. No. Product Name / Activity
3389 Bicalutamide
Non-steroidal androgen receptor antagonist
4094 Flutamide
Non-steroidal androgen receptor antagonist
6108 Galeterone
Androgen receptor antagonist; also CYP17 inhibitor

Androgen Receptor Modulators

Cat. No. Product Name / Activity
3813 TFM-4AS-1
Selective androgen receptor modulator (SARM)

Androgen Receptor Inhibitors

Cat. No. Product Name / Activity
5842 MK 386
Potent, selective human type 1 5α-reductase inhibitor

Degraders

Cat. No. Product Name / Activity
7254 ARCC 4
Potent and selective androgen receptor degrader

Other

Cat. No. Product Name / Activity
4946 AIM 100
Potent and selective Ack1 inhibitor
3293 Finasteride
Type II 5α-reductase inhibitor
3572 GSK 650394
Serum- and glucocorticoid-regulated kinase (SGK) inhibitor
2968 Spironolactone
Antiandrogen; inhibits steroid hormone biosynthesis. Also MR antagonist
6223 XY 018
Inhibits AR expression; RORγ antagonist

Androgen receptors (ARs) (also known as dihydrotestosterone receptors) are nuclear hormone receptors of the NR3C class, which also includes mineralocorticoid, progesterone and glucocorticoid receptors. They are expressed in bone marrow, mammary gland, prostate, testicular and muscle tissues where they exist as dimers coupled to Hsp90 and HMGB proteins, which are shed upon ligand binding.

Activated androgen receptors bind to nuclear response elements of the genome, with an inverted palindromic 15 nucleotide sequence, to regulate gene transcription. Androgen receptors also affect gene expression through interaction with transcription factors including AP-1, NF-κB and STAT.

Target genes of androgen receptors include insulin-like growth factor 1 (IGF-1) and genes involved in the development of primary and secondary male sexual characteristics, maintenance of sexual function and possibly have a causative role in aggressive behavior. Furthermore, androgen receptors have recently been shown to have actions that are independent of DNA interactions.

Congential mutations in androgen receptors are associated with androgen insensitivity syndromes, virility and spinal and bulbar muscular atrophy. Perturbations in androgen receptor expression is also a common feature of prostate cancer. The human gene encoding the androgen receptor has been localized to Xq11-12.

External sources of pharmacological information for Androgen Receptors :

Androgen Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human AR NM_000044 P10275
Mouse Ar NM_013476 P19091
Rat Ar NM_012502 P15207