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androgen receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (128) 5 alpha Reductase (1) Akt (2) Apoptosis (5) Aryl Hydrocarbon Receptor (3) Autophagy (15) Bacterial (1) Bcl-2 Family (2) Calcium Channel (3) Caspase (2) CXCR (1) Cytochrome P450 (3) Drug Isomer (1) Drug Metabolite (9) Endogenous Metabolite (2) Environmental Pollutants (4) Estrogen Receptor/ERR (6) Fungal (5) Gap Junction Protein (2) Glucocorticoid Receptor (3) GnRH Receptor (1) Herbicide (1) Integrin (2) Isotope-Labeled Compounds (20) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (3) Mineralocorticoid Receptor (14) NF-κB (2) NO Synthase (2) p38 MAPK (2) Parasite (3) Phosphodiesterase (PDE) (1) PI3K (2) Progesterone Receptor (2) Prostaglandin Receptor (1) PROTACs (2) PTHR (1) Pyroptosis (2) Reference Standards (18)
By Research Areas:	Cancer (110) Cardiovascular Disease (10) Endocrinology (32) Infection (10) Inflammation/Immunology (8) Metabolic Disease (15) Neurological Disease (2)
Click Chemistry:	PROTAC Synthesis (1)

148

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Androgen Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-70002

Enzalutamide Maximum Cited Publications 214 Publications Verification MDV3100	Androgen Receptor Autophagy	Cancer
Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .

HY-16985

Darolutamide 5+ Cited Publications ODM-201; BAY-1841788	Androgen Receptor	Cancer
Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a K_i of 11 nM for rat wild-type AR (wtAR) and IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-111372

Finerenone 5+ Cited Publications BAY 94-8862	Mineralocorticoid Receptor	Cardiovascular Disease Metabolic Disease
Finerenone (BAY 94-8862) is a third-generation, selective, and orally active nonsteroidal *mineralocorticoid receptor* (MR)** antagonist (IC₅₀ = 18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (> 500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-16060

Apalutamide 10+ Cited Publications ARN-509	Androgen Receptor	Cancer
Apalutamide (ARN-509) is a potent and competitive **androgen receptor** (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-14249

Bicalutamide 15+ Cited Publications	Androgen Receptor Autophagy	Cancer
Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer .

HY-15758

3,3'-Diindolylmethane 10+ Cited Publications DIM; Arundine; HB 236	Androgen Receptor Autophagy	Cancer
3,3'-Diindolylmethane is a strong, pure **androgen receptor** (AR) antagonist.

HY-13702

Nilutamide Nilandron; RU 23908	Androgen Receptor Parasite	Infection Endocrinology Cancer
Nilutamide (Nilandron) is an orally active nonsteroidal androgen receptor antagonist with affinity for androgen receptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostate cancer. Nilutamide also has antischistosomal properties .

HY-B0845

Prochloraz 1 Publications Verification BTS 40542	Environmental Pollutants Estrogen Receptor/ERR Aryl Hydrocarbon Receptor Fungal Androgen Receptor	Infection Endocrinology
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 .

HY-111372R

Finerenone (Standard) BAY 94-8862 (Standard)	Reference Standards Mineralocorticoid Receptor	Cardiovascular Disease
Finerenone (Standard) is the analytical standard of Finerenone. This product is intended for research and analytical applications. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal *mineralocorticoid receptor* (MR)** antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-130992

Androgen receptor antagonist 1	Androgen Receptor Ligands for Target Protein for PROTAC	Cancer
Androgen receptor antagonist 1 is an orally available full **androgen receptor** (AR) antagonist with an IC₅₀ of 59 nM . Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively .

HY-10561

RU 58841 PSK-3841; HMR-3841	Androgen Receptor	Endocrinology
RU 58841 (PSK-3841) is a specific **androgen receptor** antagonist or anti-androgen. RU 58841 has a dramatic effect on hair regrowth .

HY-70002B

Enzalutamide carboxylic acid 2 Publications Verification MDV3100 carboxylic acid	Drug Metabolite	Cancer
Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist .

HY-15103

AH3960	PTHR Androgen Receptor	Cancer
AH3960 (compound 16c) is an antagonist of **androgen receptor. AH3960 binds wild as well as T877** mutant type androgen receptors. AH3960 selectively inhibits T877 with an IC₅₀ value of 0.82 μM. AH3960 also serves as an agonist of *parathyroid hormone receptor-1 (PTHR1)* .

HY-130845A

AR antagonist 1 hydrochloride	Ligands for E3 Ligase Ligands for Target Protein for PROTAC Androgen Receptor	Cancer
AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020) .

HY-70002R

Enzalutamide (Standard) MDV3100 (Standard)	Reference Standards Androgen Receptor Autophagy	Cancer
Enzalutamide (Standard) is the analytical standard of Enzalutamide. This product is intended for research and analytical applications. Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .

HY-112895

UT-155 2 Publications Verification	Androgen Receptor	Cancer
UT-155 is a selective and potent androgen receptor (AR) antagonist, with a K_i of 267 nM for UT-155 binding to AR-LBD.

HY-19337

Ketodarolutamide 1 Publications Verification BAY 1896953; ORM-15341	Androgen Receptor	Cancer
Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a K_i value of 8 nM for rat wild-type AR and an IC₅₀ value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .

HY-70002S1

Enzalutamide-d6 MDV3100-d₆	Isotope-Labeled Compounds Androgen Receptor	Cancer
Enzalutamide-d₆ (MDV3100-d₆) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells .

HY-109070

Ralaniten EPI-002	Androgen Receptor	Cancer
Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC₅₀ of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC) .

HY-137448

Rezvilutamide SHR3680	Androgen Receptor	Cancer
Rezvilutamide (SHR3680) is an orally active **androgen receptor** antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer .

HY-70002S

Deutenzalutamide Enzalutamide-d₃; MDV3100-d₃	Androgen Receptor Autophagy	Cancer
Deutenzalutamide (Enzalutamide-d₃) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .

HY-108250

(R)-Bicalutamide	Androgen Receptor	Cancer
(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer .

HY-109619

D4-abiraterone Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite	Androgen Receptor Cytochrome P450	Cancer
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of **androgen receptor**.

HY-112689

Androgen receptor antagonist 9	Androgen Receptor	Endocrinology
Androgen receptor antagonist 9 (compound 28) is an antagonist of the androgen receptor .

HY-B0561R

Spironolactone (Standard) 5+ Cited Publications SC9420 (Standard)	Reference Standards Mineralocorticoid Receptor Androgen Receptor Autophagy	Metabolic Disease Cancer
Spironolactone (Standard) is the analytical standard of Spironolactone. This product is intended for research and analytical applications. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC₅₀ of 24 nM. Spironolactone is also a potent antagonist of **androgen receptor with an IC₅₀ of 77 nM. Spironolactone promotes autophagy** in podocytes .

HY-15758R

3,3'-Diindolylmethane (Standard) DIM (Standard); Arundine (Standard); HB 236 (Standard)	Reference Standards Androgen Receptor Autophagy	Cancer
3,3'-Diindolylmethane (Standard) is the analytical standard of 3,3'-Diindolylmethane. This product is intended for research and analytical applications. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.

HY-141487

CLP-3094 2 Publications Verification	Androgen Receptor	Metabolic Disease Inflammation/Immunology
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC₅₀=4 μM) . CLP-3094 is a selective, potent GPR142 antagonist .

HY-16985S

Darolutamide-d4 ODM-201-d₄; BAY-1841788-d₄	Isotope-Labeled Compounds Androgen Receptor	Cancer
Darolutamide-d₄ (ODM-201-d₄) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a K_i of 11 nM for rat wild-type AR (wtAR) and an IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-136596

Apalutamide-COOH	Drug Metabolite	Cancer
Apalutamide-COOH is a metabolite of Apalutamide. Apalutamide is a potent and competitive **androgen receptor** (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-13607

BMS-641988	Androgen Receptor	Cancer
BMS-641988 (compound 23) is an oral active nonsteroidal **androgen receptor** antagonist with the K_i of 1.7 nM. BMS-641988 shows anticancer activity .

HY-152524

Androgen receptor antagonist 7	Androgen Receptor	Cancer
Androgen receptor antagonist 7 is an effective **androgen receptor** (AR) antagonist with an IC₅₀ value of 1.18 µM. Androgen receptor antagonist 7 has biological activity in vitro and inhibits the expression of AR target in a time and dose dependent manner with an GI₅₀ value of 7.9 µM .

HY-121094

Androgen receptor allosteric antagonist 1	Estrogen Receptor/ERR	Cancer
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the K_i of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .

HY-16985R

Darolutamide (Standard) ODM-201 (Standard); BAY-1841788 (Standard)	Reference Standards Androgen Receptor	Cancer
Darolutamide (Standard) is the analytical standard of Darolutamide (HY-16985). This product is intended for research and analytical applications. Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a K_i of 11 nM for rat wild-type AR (wtAR) and an IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-16060S

Apalutamide-d4 ARN-509-d₄	Androgen Receptor	Cancer
Apalutamide-d₄ is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-B0561S1

Spironolactone-d3 SC9420-d₃	Isotope-Labeled Compounds Mineralocorticoid Receptor Androgen Receptor Autophagy	Metabolic Disease Cancer
Spironolactone-d₃ is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC₅₀ of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC₅₀ of 77 nM. Spironolactone promotes autophagy in podocytes .

HY-130845

AR antagonist 1	Ligands for E3 Ligase Ligands for Target Protein for PROTAC	Cancer
AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).

HY-16060S1

Apalutamide-d3 ARN-509-d₃	Androgen Receptor	Cancer
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 .

HY-111372A

(Rac)-Finerenone (Rac)-BAY 94-8862	Mineralocorticoid Receptor	Cardiovascular Disease
(Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold) .

HY-B2058

Triticonazole	Fungal Androgen Receptor	Infection
Triticonazole is an orally active triazole fungicide and androgen receptor antagonist. Triticonazole inhibits testosterone-induced androgen receptor activation and reduces basal testosterone secretion. Prenatal exposure to Triticonazole causes shortened anogenital distance in male rat fetuses and induces organ-specific histopathological changes in pigs. Triticonazole can be used for detoxification of seeds contaminated with fungal pathogens, but there is a risk of animal poisoning if the treated seeds are used as animal feed .

HY-14250

PF-998425	Androgen Receptor	Endocrinology
PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC₅₀ of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research .

HY-B1986S

p,p'-DDE-d8 4,4'-DDE-d₈; p,p'-Dichlorodiphenyldichloroethylene-d₈	Androgen Receptor Drug Metabolite	Endocrinology
p,p'-DDE-d₈ is the deuterium labeled p,p'-DDE . p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC₅₀ of 5 μM and a K_i of 3.5 μM .

HY-111372S

Finerenone-d3 BAY 94-8862-d₃	Mineralocorticoid Receptor	Others
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal *mineralocorticoid receptor* (MR)** antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-153772

Androgen receptor antagonist 8	Androgen Receptor	Cancer
Androgen receptor antagonist 8 (Example 13) is an **androgen receptor** antagonist. Androgen receptor antagonist 8 inhibits prostate specific antigen secretion in LNcap cell (IC₅₀: 88 nM). Androgen receptor antagonist 8 can be used for prostate cancer research .

HY-160659

Androgen receptor antagonist 10	Androgen Receptor	Endocrinology
Androgen receptor antagonist 10 (compound 6h) is a **androgen receptor** antagonist. Androgen receptor antagonist 10 reduces the wax esters in the golden syrian hamster model .

HY-146026

Androgen receptor antagonist 3	Androgen Receptor	Cancer
Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC₅₀ of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities .

HY-172908

Androgen receptor antagonist 13	Androgen Receptor	Cancer
Androgen receptor antagonist 13 (compound 8a) is an orally active **Androgen receptor** antagonist with an IC₅₀ of 0.20 μM. Androgen receptor antagonist 13 can be used in the study of prostate cancer .

HY-169349

Androgen receptor antagonist 12	Androgen Receptor	Cancer
Androgen receptor antagonist 12 (Compound EF2) is an orally active **Androgen receptor** (AR) antagonist (IC₅₀: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .

HY-146027

Androgen receptor antagonist 4	Androgen Receptor	Cancer
Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC₅₀ of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities .

HY-146494

Androgen receptor antagonist 5	Androgen Receptor	Cancer
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC₅₀ value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .

HY-168141

Androgen receptor antagonist 11	Androgen Receptor	Cancer
Androgen receptor antagonist 11 (compund N29) is a derivative of the androgen receptor (AR) antagonist M17-B15, and is a selective and orally active AR antagonist (IC₅₀=18 nM). .

Cat. No.	Product Name	Target	Research Area

HY-P2446

ORG 30276 APTAA-LHRH	GnRH Receptor	Endocrinology
ORG 30276 (APTAA-LHRH) is a potent GnRH antagonist that effectively reduces serum LH and FSH levels in male rats. ORG 30276 significantly decreases unoccupied pituitary GnRH receptors, leading to suppressed gonadotropin secretion. ORG 30276 treatment results in a considerable reduction in mRNA levels of gonadotropin beta-subunits in the pituitary gland. ORG 30276's effects on gonadotropin dynamics can be selectively reversed by the replacement of specific sex steroids, with androgens being particularly effective for the FSH beta-subunit mRNA levels.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-15758

3,3'-Diindolylmethane 10+ Cited Publications DIM; Arundine; HB 236	Alkaloids other families Classification of Application Fields Plants Disease Research Fields Alkaloid Dimers Source Classification Cancer	Androgen Receptor Autophagy
3,3'-Diindolylmethane is a strong, pure **androgen receptor** (AR) antagonist.

HY-N2908

Atraric acid Methyl atrarate	Structural Classification Microorganisms Classification of Application Fields Phenols Essence, Fragrance Cosmetic Research Plants Inflammation/Immunology Disease Research Fields Cancer	Environmental Pollutants NF-κB Androgen Receptor p38 MAPK NO Synthase
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 .

HY-N0475

Triptophenolide Hypolide; (+)-Triptophenolide	Structural Classification Monophenols Classification of Application Fields Terpenoids Celastraceae Other Diseases Phenols Diterpenoids Tripterygium wilfordii Hook. f. Plants Disease Research Fields Source Classification	Androgen Receptor Pyroptosis Caspase Bcl-2 Family Apoptosis
Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC₅₀ of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .

HY-15758R

3,3'-Diindolylmethane (Standard) DIM (Standard); Arundine (Standard); HB 236 (Standard)	Alkaloids Structural Classification other families Plants Alkaloid Dimers Source Classification	Reference Standards Androgen Receptor Autophagy
3,3'-Diindolylmethane (Standard) is the analytical standard of 3,3'-Diindolylmethane. This product is intended for research and analytical applications. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.

HY-N9917

Galloylalbiflorin 6′-O-Galloylalbiflorin	Paeonia lactiflora Pall. Polyphenols Plants Paeoniaceae Source Classification	Androgen Receptor
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 .

HY-W087006

p-Hydroxyphenylacetone	Structural Classification Other Monoterpenes Terpenoids Sargentodoxa cuneata (Oliv.) Rehd. et Wils. Plants Sargentodoxaceae Source Classification	Androgen Receptor
p-Hydroxyphenylacetone, a Raspberry ketone (HY-N1426) derivative, is an androgen receptor (AR) antagonist with an IC₅₀ of 420 μM in MDA-kb2 human breast cancer cells. p-Hydroxyphenylacetone can be used for breast cancer research .

HY-N2908R

Atraric acid (Standard) Methyl atrarate (Standard)	Microorganisms Phenols Plants	Reference Standards Androgen Receptor NO Synthase p38 MAPK NF-κB
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].

HY-N0475R

Triptophenolide (Standard) Hypolide (Standard); (+)-Triptophenolide (Standard)	Structural Classification Monophenols Terpenoids Celastraceae Phenols Diterpenoids Tripterygium wilfordii Hook. f. Plants Source Classification	Reference Standards Androgen Receptor Pyroptosis Caspase Bcl-2 Family Apoptosis
Triptophenolide (Standard) (Hypolide) is the analytical standard of Triptophenolide (HY-N0475). This product is intended for research and analytical applications. Triptophenolide is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC₅₀ of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .

HY-W585917

Bisphenol F bis(2-chloro-1-propanol) ether BFDGE·2HCl	Structural Classification Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Androgen Receptor
Bisphenol F bis(2-chloro-1-propanol) ether (BFDGE·2HCl) is an **androgen receptor** antagonist with a human IC₅₀ of 18 μM. Bisphenol F bis(2-chloro-1-propanol) ether binds to the androgen receptor. Bisphenol F bis(2-chloro-1-propanol) ether (BFDGE·2HCl) can be used for research on hormonal activity .

Cat. No.	Product Name	Chemical Structure

HY-70002S1

Enzalutamide-d6
Enzalutamide-d₆ (MDV3100-d₆) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells .

HY-70002S

Deutenzalutamide
Deutenzalutamide (Enzalutamide-d₃) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .

HY-16985S

Darolutamide-d4

Darolutamide-d₄ (ODM-201-d₄) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a K_i of 11 nM for rat wild-type AR (wtAR) and an IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-16060S

Apalutamide-d4
Apalutamide-d₄ is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-B0561S1

Spironolactone-d3
Spironolactone-d₃ is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC₅₀ of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC₅₀ of 77 nM. Spironolactone promotes autophagy in podocytes .

HY-B1866S

Linuron-d6

Linuron-d₆ is the deuterium labeled Linuron (HY-B1866). Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor .

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 .

HY-B1986S

p,p'-DDE-d8
p,p'-DDE-d₈ is the deuterium labeled p,p'-DDE . p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC₅₀ of 5 μM and a K_i of 3.5 μM .

HY-111372S

Finerenone-d3

Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-111372S1

Finerenone-d5

1 Publications Verification

Finerenone-d₅ (BAY 94-8862-d₅) is deuterium labeled Finerenone. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .

HY-W754151

N-Desmethyl apalutamide-d4

N-Desmethyl apalutamide-d₄ is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .

HY-B0561S

Spironolactone-d7
Spironolactone-d₇ is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC₅₀ of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC₅₀ of 77 nM. Spironolactone promotes autophagy in podocytes .

HY-14249S

Bicalutamide-d4
Bicalutamide-d₄ is the deuterium labeled Bicalutamide. Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer .

HY-16060S3

Apalutamide-d7
Apalutamide-d₇ is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive **androgen receptor** (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-16060S2

Apalutamide-13C,d3
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 .

HY-B0251S

Eplerenone-d3
Eplerenone-d₃ is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC₅₀ of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch .

HY-B0561S4

Spironolactone-d6-1

Spironolactone-d₆-1 is the deuterium labeled Spironolactone (HY-B0561). Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC₅₀=24 nM) and androgen receptor (IC₅₀=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (Ang II)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type II diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca ²⁺ channels to exert antihypertensive effects .

HY-B0561S2

Spironolactone-d3-1
Spironolactone-d₃-1 is deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC₅₀ of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC₅₀ of 77 nM. Spironolactone promotes autophagy in podocytes .

HY-14249S1

(R)-Bicalutamide-d5
(R)-Bicalutamide-d₅ is deuterated labeled (R)-Bicalutamide (HY-108250). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer .

HY-W753141

p,p'-DDE-13C12
p,p'-DDE- ¹³C₁₂ is ¹³C labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent **androgen receptor** antagonist, with an IC₅₀ of 5 μM and a K_i of 3.5 μM .

HY-W716464

Prochloraz-d7
Prochloraz-d₇ (BTS 40542-d₇) is the deuterium labeled Prochloraz (HY-B0845). 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 .

HY-135331S

N-Desmethyl-Apalutamide-15N,d4

N-Desmethyl-Apalutamide-15N,d4 is the ¹⁵N and deuterium labeled isotope of N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .

HY-19337S1

Ketodarolutamide-d6

Ketodarolutamide-d₆ (BAY 1896953-d₆) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a K_i value of 8 nM for rat wild-type AR and an IC₅₀ value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .

HY-19337S

Ketodarolutamide-d3

Ketodarolutamide-d₃ (BAY 1896953-d₃) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a K_i value of 8 nM for rat wild-type AR and an IC₅₀ value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .

HY-W950003

(Rac)-Finerenone-d5

(Rac)-Finerenone-d₅ ((Rac)-BAY 94-8862-d₅) is the deuterium labeled (Rac)-Finerenone (HY-111372A). (Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).

Cat. No.	Product Name		Classification

HY-114402

ARD-69		PROTAC Synthesis
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC) . ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).

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