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Results for "

androgen receptor modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (32) 5 alpha Reductase (1) Adrenergic Receptor (2) Akt (1) Antibiotic (1) Apoptosis (3) Bacterial (1) Caspase (1) Drug Isomer (1) ERK (1) Estrogen Receptor/ERR (3) Glucocorticoid Receptor (1) GSK-3 (1) Isotope-Labeled Compounds (1) JNK (1) Neprilysin (1) NF-κB (1) PI3K (1) PPAR (2) Reference Standards (4) ROR (1)
By Research Areas:	Cancer (21) Cardiovascular Disease (2) Endocrinology (10) Infection (1) Inflammation/Immunology (4) Metabolic Disease (9) Neurological Disease (7)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Androgen Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13273

Ostarine 3 Publications Verification MK-2866; GTX-024; Enobosarm	Androgen Receptor	Others Cancer
Ostarine (MK-2866) is a selective androgen receptor modulator (SARMs) that regulates cardiomyocyte function, improves bone healing, regulates uterine function, and influences muscle tissue metabolism .

HY-14383

Vosilasarm 5+ Cited Publications RAD140; EP0062	Androgen Receptor	Neurological Disease Endocrinology Cancer
Vosilasarm (RAD140) is a potent, orally active, nonsteroidal selective **androgen receptor** modulator (SARM) with a K_i of 7 nM. Vosilasarm shows good selectivity over other steroid hormone nuclear receptors .

HY-100186

GSK-2881078 5 Publications Verification	Androgen Receptor	Cardiovascular Disease Others Metabolic Disease Inflammation/Immunology Endocrinology Cancer
GSK-2881078 is an orally active and nonsteroidal selective **androgen receptor** modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)₂ cells (EC₅₀ = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness .

HY-114530

LY2452473 Maximum Cited Publications 7 Publications Verification	Androgen Receptor	Metabolic Disease Cancer
LY2452473 is an orally bioavailable, selective **androgen receptor** modulator (SARM).

HY-11027

MK-0773 4 Publications Verification PF-05314882	Androgen Receptor	Endocrinology
MK-0773 is a *selective androgen* receptor modulators (SARMs) that binds to AR with an IC₅₀** of 6.6 nM.

HY-122025

AC-262536 1 Publications Verification	Androgen Receptor	Metabolic Disease
AC-262536 is a selective and non-steroidal **androgen receptor** modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM) .

HY-112256

ACP-105 5+ Cited Publications	Androgen Receptor	Inflammation/Immunology
ACP-105 is an orally available, selective amd potent **androgen receptor** modulator (SARM), with pEC₅₀s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.

HY-12023

GTx-007 4 Publications Verification S-4	Androgen Receptor	Cancer
GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with K_i of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity .

HY-100348

EPI-001	Androgen Receptor PPAR Apoptosis	Cancer
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC₅₀ of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .

HY-N3755

Dihydroresveratrol	Estrogen Receptor/ERR	Cancer
Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations .

HY-112257

S-23 1 Publications Verification	Androgen Receptor	Metabolic Disease
S-23 is an orally active selective **androgen receptor** modulator (SARM) with a K_i of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats .

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-18102

GLPG0492 Maximum Cited Publications 7 Publications Verification	Androgen Receptor	Neurological Disease
GLPG0492 is an orally active, non-steroidal selective **androgen receptor** modulator. GLPG0492 exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .

HY-103246

TFM-4AS-1	Androgen Receptor	Cancer
TFM-4AS-1 is a *selective androgen* receptor modulator (SARM)*, and a potent androgen* receptor (AR) ligand with an IC₅₀ of 38 nM. TFM-4AS-1 is a gene-selective agonist .

HY-45509

TLB 150 Benzoate RAD150	Androgen Receptor	Neurological Disease
TLB 150 Benzoate (RAD150) is a nonsteroidal **androgen receptor** modulator with an IC₅₀ value of 0.13 μM. TLB 150 Benzoate spontaneously cyclizes under physiological conditions to form RAD 179, resulting in a persistent, reversible, and slow neuronal conduction blockade. TLB 150 Benzoate can be used for research on neurological diseases .

HY-135319

Strictinin	Bacterial Antibiotic ERK JNK NF-κB ROR Apoptosis Caspase GSK-3 Akt PI3K	Infection Metabolic Disease Inflammation/Immunology Cancer
Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1 .

HY-171048

GTx-027	Androgen Receptor	Endocrinology Cancer
GTx-027 is an orally active and non-steroidal selective **androgen receptor** modulator (SARM). GTx-027 shows androgen receptor (AR) transactivation effects with the EC50 of 1.8 nM. GTx-027 acts selectively increase muscle weight (anabolic) without affecting secondary sexual organs (androgenic). GTx-027 has the protential for the study of breast cancer and stress urinary incontinence (SUI) .

HY-103576

LGD-3303 4 Publications Verification	Androgen Receptor	Endocrinology
LGD-3303 is a selective androgen receptor modulator (SARM).

HY-W744216

Trestolone acetate	Androgen Receptor	Metabolic Disease
Trestolone acetate is an androgenic steroid. Trestolone acetate binds to Sugammadex sodium (HY-B0079), reducing the ability of Sugammadex sodium to reverse amino steroid neuromuscular blocking agents .

HY-18102A

GLPG0492 (R enantiomer)	Drug Isomer Androgen Receptor	Neurological Disease
GLPG0492 R enantiomer is the R enantiomer of GLPG0492. GLPG0492 is an orally active, non-steroidal selective **androgen receptor** modulator.

HY-139046

MEPB	Adrenergic Receptor	Neurological Disease
MEPB is a modulator of AF-2 of the androgen receptor. MEPB increases co-repressor binding of AR. MEPB can bind to the BF3 pocket of AR specifically, thereby modulating the binding of co-regulators to the AF2 domain. MEPB alleviates degeneration in spinal bulbar muscular atrophy mouse model .

HY-125065

MK-4541	Androgen Receptor 5 alpha Reductase	Endocrinology Cancer
MK-4541 is an orally active and selective **androgen receptor** (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model .

HY-171049

Androgen receptor modulator 3	Androgen Receptor	Cardiovascular Disease
Androgen receptor modulator 3 is a selective modulator for **androgen receptor** that can be used for research of sarcopenia .

HY-105318

LGD-2226	Androgen Receptor	Metabolic Disease Endocrinology
LGD-2226 is a selective and orally active **androgen receptor** modulator with an EC₅₀ of 0.2 nM and a K_i of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction .

HY-114154

AL-438	Glucocorticoid Receptor	Inflammation/Immunology
AL-438 is a potent, selective and orally active glucocorticoid receptor modulator with K_is of 2.5, 1786, 53, 1440, >1000 nM for glucocorticoid receptor, progesterone receptor, mineralocorticoid receptor, androgen receptor, estrogen receptor, respectively. AL-438 shows antiinflammatory activity .

HY-103578

S-40503	Androgen Receptor	Cancer
S-40503 is an orally active and selective **androgen receptor** modulator. S-40503 significantly increases the bone mineral density (BMD) and biomechanical strength of femoral cortical bone .

HY-103577

LG-121071	Androgen Receptor	Cancer
LG-121071 is an orally active and selective **androgen receptor** modulator with a K_i of 17 nM .

HY-111246

MK-3984	Androgen Receptor	Cancer
MK-3984 is a *selective androgen* receptor modulator (SARM)**. MK-3984 can be used for the research of muscle wasting associated with cancer .

HY-111044

(+)-JNJ-37654032	Androgen Receptor	Cancer
(+)-JNJ-37654032 is an orally active and selective **androgen receptor** modulator. (+)-JNJ-37654032 can be used in the study of muscle-wasting diseases .

HY-111309

LGD-2941	Androgen Receptor	Endocrinology
LGD-2941 is an orally active, potent and selective **androgen receptor** modulator. LGD-2941 shows excellent anabolic activity in muscle with reduced effect on the prostate in a rat model of hypogonadism. LGD-2941 also improves bone strength in a rat model of post-menopausal osteoporosis .

HY-123664

Trioxifene mesylate LY133314	Estrogen Receptor/ERR	Cancer
Trioxifene mesylate (LY133314) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC₅₀ of 203.49 nM and K_i of 20.84 nM. Trioxifene mesylate binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene mesylate can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma .

HY-100348R

EPI-001 (Standard)	Reference Standards Androgen Receptor PPAR Apoptosis	Cancer
EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC₅₀ of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .

HY-164477

FL442	Androgen Receptor	Cancer
FL442 is an **Androgen Receptor** (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .

HY-18102BS

GLPG0492-13C,d3 racemate	Isotope-Labeled Compounds Adrenergic Receptor	Neurological Disease
GLPG0492- ¹³C,d₃ racemate is ¹³C-labeled GLPG0492 (racemate) (HY-18102B). GLPG0492 racemate is an orally active, non-steroidal selective **androgen receptor** modulator. GLPG0492 racemate exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 racemate effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 racemate prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .

HY-103576R

LGD-3303 (Standard)	Reference Standards Androgen Receptor	Endocrinology
LGD-3303 (Standard) is the analytical standard of LGD-3303 (HY-103576). This product is intended for research and analytical applications. LGD-3303 is a selective androgen receptor modulator (SARM).

HY-105318R

LGD-2226 (Standard)	Reference Standards Androgen Receptor	Metabolic Disease Endocrinology
LGD-2226 (Standard) is the analytical standard of LGD-2226 (HY-105318). This product is intended for research and analytical applications. LGD-2226 is a selective and orally active androgen receptor modulator with an EC₅₀ of 0.2 nM and a K_i of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction .

HY-108250R

(R)-Bicalutamide (Standard)	Reference Standards Androgen Receptor	Cancer
(R)-Bicalutamide (Standard) is the analytical standard of (R)-Bicalutamide (HY-108250). This product is intended for research and analytical applications. (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-135529

Trioxifene LY133314 free base	Estrogen Receptor/ERR	Cancer
Trioxifene (LY133314 free base) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC₅₀ of 203.49 nM and K_i of 20.84 nM. Trioxifene binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma .

HY-156059

NEP28	Androgen Receptor Neprilysin	Neurological Disease Metabolic Disease
NEP28 is a selective **androgen receptor** modulator with an EC₅₀ of 2.90 nM in 22RV1 cells. NEP28 increases the activity of Aβ-degrading enzyme neprilysin. NEP28 is efficacious in muscle and brain without serious side effects on prostate in rats. NEP28 can be used for osteoporosis, sarcopenia, and Alzheimer's disease research .

Cat. No.	Product Name

HY-L935

Molecular Glue POI binding Fragment library	1039 compounds
POI (Protein of Interest) refers to the target protein, namely the disease-causing protein or key functional protein that undergoes degradation or functional modulation in molecular glue-mediated processes. The Molecular Glue POI Library consists of a series of fragments that can specifically bind to different types of POIs. As key components of molecular glues, these ligands form stable interactions with target proteins, laying the foundation for molecular glues to induce the interaction between POIs and E3 ubiquitin ligases. The covered POIs include various types such as cancer-associated GSPT1, androgen receptors, and abnormally aggregated proteins linked to neurodegenerative diseases. This fragment library can be applied to the screening and optimization of targeted protein degraders. By screening ligands with high affinity and strong selectivity for specific POIs from the library, core structures can be identified to develop novel molecular glues. For instance, optimization of ligands targeting GSPT1 has yielded molecular glue degraders with enhanced degradation activity. Since many POIs are difficult to drug due to the lack of traditional small-molecule binding pockets, some ligands in the POI Ligand Library can modulate such POIs by inducing protein-protein interactions, thereby further expanding the scope of drug discovery for undruggable targets. MCE has compiled a POI Fragment Library comprising thousands of POI fragments with molecular weights ranging from 150 to 400. This compound library can be widely applied in Molecular Glue research and development.

Molecular Glue POI binding Fragment library

1039 compounds

POI (Protein of Interest) refers to the target protein, namely the disease-causing protein or key functional protein that undergoes degradation or functional modulation in molecular glue-mediated processes. The Molecular Glue POI Library consists of a series of fragments that can specifically bind to different types of POIs. As key components of molecular glues, these ligands form stable interactions with target proteins, laying the foundation for molecular glues to induce the interaction between POIs and E3 ubiquitin ligases. The covered POIs include various types such as cancer-associated GSPT1, androgen receptors, and abnormally aggregated proteins linked to neurodegenerative diseases.

This fragment library can be applied to the screening and optimization of targeted protein degraders. By screening ligands with high affinity and strong selectivity for specific POIs from the library, core structures can be identified to develop novel molecular glues. For instance, optimization of ligands targeting GSPT1 has yielded molecular glue degraders with enhanced degradation activity. Since many POIs are difficult to drug due to the lack of traditional small-molecule binding pockets, some ligands in the POI Ligand Library can modulate such POIs by inducing protein-protein interactions, thereby further expanding the scope of drug discovery for undruggable targets.

MCE has compiled a POI Fragment Library comprising thousands of POI fragments with molecular weights ranging from 150 to 400. This compound library can be widely applied in Molecular Glue research and development.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N3755

Dihydroresveratrol	Human Gut Microbiota Metabolites Classification of Application Fields Phenols Polyphenols Plants Endogenous metabolite Disease Research Fields Dioscorea bulbifera Linn. Dioscoreaceae Source Classification Cancer	Estrogen Receptor/ERR
Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations .

HY-135319

Strictinin	Structural Classification Phenols Polyphenols Camellia sinensis (L.) O. Ktze. Plants Source Classification Theaceae	Bacterial Antibiotic ERK JNK NF-κB ROR Apoptosis Caspase GSK-3 Akt PI3K
Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1 .

Cat. No.	Product Name	Chemical Structure

HY-18102BS

GLPG0492-13C,d3 racemate
GLPG0492- ¹³C,d₃ racemate is ¹³C-labeled GLPG0492 (racemate) (HY-18102B). GLPG0492 racemate is an orally active, non-steroidal selective **androgen receptor** modulator. GLPG0492 racemate exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 racemate effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 racemate prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .

GLPG0492-13C,d3 racemate

GLPG0492- ¹³C,d₃ racemate is ¹³C-labeled GLPG0492 (racemate) (HY-18102B). GLPG0492 racemate is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 racemate exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 racemate effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 racemate prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy .

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