Androgen Receptors

ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.

MK-0773, one of selective androgen receptor modulators (SARMs), is a 4-aza-steroid that exhibited tissue selectivity in humans (IC50= 6.6 nM).

CSRM617 Hydrochloride is an inhibitor of the transcription factor ONECUT2 (OC2), thereby suppressing metastasis in mice.

Proxalutamide (GT0918) is a potent androgen receptor (AR) antagonist.

Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs.

Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status.

ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80?nM and 22 nM, respectively.

UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.

GLPG0492 is a novel selective androgen receptor modulator; exhibited anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate after oral dosing.

(R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer.