Androgen Receptor

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S2840 Apalutamide (ARN-509) <1 mg/mL 18 mg/mL 5 mg/mL
S4797 Nicergoline -1 mg/mL 22 mg/mL -1 mg/mL
S1304 Megestrol Acetate <1 mg/mL 33 mg/mL 15 mg/mL
S7040 AZD3514 <1 mg/mL 100 mg/mL 100 mg/mL
S1250 Enzalutamide (MDV3100) <1 mg/mL 92 mg/mL <1 mg/mL
S1190 Bicalutamide <1 mg/mL 86 mg/mL 5 mg/mL
s9045 Triptophenolide -1 mg/mL 62 mg/mL -1 mg/mL
S5285 RU58841 <1 mg/mL 73 mg/mL 73 mg/mL
S4836 Nilutamide <1 mg/mL 63 mg/mL 63 mg/mL
S2803 Galeterone <1 mg/mL 24 mg/mL 40 mg/mL
S1908 Flutamide <1 mg/mL 55 mg/mL 55 mg/mL
S2604 Dehydroepiandrosterone (DHEA) <1 mg/mL 57 mg/mL 57 mg/mL
S2042 Cyproterone Acetate <1 mg/mL 83 mg/mL 10 mg/mL
S4054 Spironolactone <1 mg/mL 83 mg/mL 20 mg/mL
S4593 Chlormadinone acetate <1 mg/mL 27 mg/mL 1 mg/mL
S7559 Darolutamide (ODM-201) <1 mg/mL 80 mg/mL 38 mg/mL
S7955 EPI-001 <1 mg/mL 79 mg/mL 79 mg/mL
S1140 Andarine <1 mg/mL 88 mg/mL 88 mg/mL
S4794 Drostanolone Propionate -1 mg/mL 18 mg/mL -1 mg/mL
S4795 Trenbolone acetate -1 mg/mL 62 mg/mL -1 mg/mL
S2832 Epiandrosterone <1 mg/mL 29 mg/mL 58 mg/mL
S3946 Mesterolone -1 mg/mL 13 mg/mL -1 mg/mL
S3717 Testosterone Enanthate 9 mg/mL 80 mg/mL 80 mg/mL
S4757 Dihydrotestosterone(DHT) <1 mg/mL 58 mg/mL 58 mg/mL
S1174 Ostarine (GTx-024, MK-2866 ) <1 mg/mL 78 mg/mL 78 mg/mL
S5275 Testolone (RAD140) -1 mg/mL 78 mg/mL -1 mg/mL
Catalog No. Information Product Use Citations Product Validations

Apalutamide (ARN-509)

Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.



Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has a selective alpha-1A adrenergic receptor blocking property and also other additional mechanisms of actions.


Megestrol Acetate

Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.



AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.


Enzalutamide (MDV3100)

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.



Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.



Triptophenolide, derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.



RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.



Nilutamide is a nonsteroidal antiandrogen (NSAA) with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). It is used in the treatment of prostate cancer.



Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.



Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.


Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.


Cyproterone Acetate

Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.



Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.


Chlormadinone acetate

Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.


Darolutamide (ODM-201)

Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.



EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.



Andarine is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.


Drostanolone Propionate

Drostanolone Propionate is an anabolic androgenic steroid with strong anti-estrogenic properties.


Trenbolone acetate

Trenbolone acetate, a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.



Protodioscin, a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.



Epiandrosterone is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.



Mesterolone is a synthetic steroid with anabolic and androgenic activities.


Testosterone Enanthate

Testosterone Enanthate is an androgen and anabolic steroid used in androgen replacement therapy.


Boldenone Undecylenate

Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic.



Dihydrotestosterone is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.


Ostarine (GTx-024, MK-2866 )

MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.


Testolone (RAD140)

RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.