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Androgen Receptor Antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (95) 5 alpha Reductase (1) Apoptosis (2) Aryl Hydrocarbon Receptor (2) Autophagy (14) Bacterial (1) Calcium Channel (2) CXCR (1) Cytochrome P450 (3) Drug Metabolite (6) Endogenous Metabolite (1) Estrogen Receptor/ERR (5) Fungal (2) Glucocorticoid Receptor (2) GnRH Receptor (1) Isotope-Labeled Compounds (12) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (4) Mineralocorticoid Receptor (11) NF-κB (2) NO Synthase (2) p38 MAPK (2) Parasite (3) Phosphodiesterase (PDE) (1) Progesterone Receptor (1) PROTACs (1) PTHR (1)
By Research Areas:	Cancer (83) Cardiovascular Disease (7) Endocrinology (27) Infection (6) Inflammation/Immunology (5) Metabolic Disease (9)
Click Chemistry:	PROTAC Synthesis (1)

112

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Androgen Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112689

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

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-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-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-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-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). .

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-157455

AR antagonist 5	Androgen Receptor	Cancer
AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC₅₀ value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure ^[1.

HY-118409

VPC-3033	Androgen Receptor	Endocrinology Cancer
VPC-3033 is an **androgen receptor** antagonist. VPC-3033 has a strong androgen DHT replacement potency (IC₅₀: 0.625-2.5 μM), can effectively inhibit androgen receptor transcriptional activity (IC₅₀=0.3 μM), and has a strong androgen receptor degradation ability. In addition, VPC-3033 exhibits significant anti-androgen receptor activity against prostate cancer cells resistant to Enzalutamide (HY-70002) .

HY-173640

ID11916	Androgen Receptor Phosphodiesterase (PDE)	Cancer
ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3 .

HY-160692

AR antagonist 7	Androgen Receptor	Others
AR antagonist 7 (86) is an androgen receptor (AR) antagonist that can be used in the research of hair loss .

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-15758

3,3'-Diindolylmethane 5+ Cited Publications DIM; Arundine; HB 236	Androgen Receptor Autophagy	Cancer
3,3'-Diindolylmethane is a strong, pure **androgen receptor** (AR) antagonist.

HY-105122

Zanoterone WIN 49596	Androgen Receptor	Endocrinology Cancer
Zanoterone is an orally active antagonist of the androgen receptor (AR) with a K_i of 2.2 μM. Zanoterone blocks the binding of androgens such as testosterone and dihydrotestosterone (DHT), inhibiting the androgen signaling pathway, thereby reducing androgen-dependent prostate hyperplasia and prostate cancer growth .

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-163485

AR antagonist 8	Androgen Receptor	Endocrinology
AR antagonist 8 (compound 16), an unnatural entestrane, is a potent Lupeol-inspired androgen receptor (AR) antagonist with an IC₅₀ of 0.76 μM .

HY-N9917

Galloylalbiflorin 6′-O-Galloylalbiflorin	Androgen Receptor	Endocrinology Cancer
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-W041703

6-Amino-5-bromoquinoxaline 5-Bromoquinoxalin-6-amine	Androgen Receptor	Others
6-Amino-5-bromoquinoxaline is a 2-(arylamino)imidazole derivative and a precursor of α1- and α2-androgen *receptor* antagonists .

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-172612

AR antagonist 13	Androgen Receptor	Cancer
AR antagonist 13 (compound 19) is an **androgen receptor** antagonist with inhibition rates exceeding 71.5% at 10 μM. AR antagonist 13 inhibits prostate cancer cell growth .

HY-13702R

Nilutamide (Standard)	Androgen Receptor Parasite	Infection Endocrinology Cancer
Nilutamide (Standard) is the analytical standard of Nilutamide. This product is intended for research and analytical applications. 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-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-14249

Bicalutamide 10+ 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-70002B

Enzalutamide carboxylic acid 1 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-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-142923

AR antagonist 2	Androgen Receptor	Cancer
AR antagonist 2 (compound 58) is a potent androgen receptor (AR) inhibitor with an IC₅₀ of 0.95 μM. AR antagonist 2 has the potential for cancer research .

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-16985

Darolutamide 5 Publications Verification ODM-201; BAY-1841788	Androgen Receptor	Cancer
Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC₅₀ of 26 nM in in vitro assay.

HY-70002

Enzalutamide Maximum Cited Publications 168 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-164371

(+)-JJ-74-138	Androgen Receptor	Cancer
(+)-JJ-74-138, a novel non-competitive androgen receptor (AR) antagonist, is capable of inhibiting Enzalutamide-resistant CRPC .

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-123310

JNJ-26146900	Androgen Receptor	Cancer
JNJ-26146900 is a potent and orally active **androgen receptor** antagonist with a K_i value of 400nM for rat AR. JNJ-26146900 is a nonsteroidal androgen receptor (AR) ligand. JNJ-26146900 reduces prostate tumor size and prevents bone loss. JNJ-26146900 can be used in research of cancer .

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-160680

AR antagonist 6	Androgen Receptor	Endocrinology
AR antagonist 6 (compound 6i) is a diphenyl ether androgen receptor (AR) antagonist that binds AR at a concentration of 120 nM. AR antagonist 6 exhibits low toxicity and in vitro activity against the golden Syrian hamster ear model .

HY-B0561S1

Spironolactone-d3 SC9420-d₃	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[1][2][3].

HY-B0561S

Spironolactone-d7 SC9420-d₇	Isotope-Labeled Compounds Mineralocorticoid Receptor Androgen Receptor Autophagy Calcium Channel	Metabolic Disease Cancer
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[1][2][3].

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[1].

HY-W013272

Hydroxyflutamide HFT	Androgen Receptor	Cancer
Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent **androgen receptor** antagonist (IC₅₀=700 nM). Hydroxyflutamide can be used for the research of prostate cancer .

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-151266

AR antagonist 4	Androgen Receptor	Cancer
AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist with an IC₅₀ of 246.6 nM against wt-AR, and is also an AR degrader with a DC₅₀ of 2.84 μM .

HY-B0561S2

Spironolactone-d3-1 SC9420-d₃-1	Isotope-Labeled Compounds Mineralocorticoid Receptor Androgen Receptor Autophagy	Metabolic Disease Cancer
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[1][2][3].

HY-125839

OP-3633	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
OP-3633 is a potent and selective steroidal *glucocorticoid receptor* (GR)** antagonist with an IC₅₀ of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism .

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-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-B0561R

Spironolactone (Standard) 3 Publications Verification SC9420 (Standard)	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-144127

AR antagonist 3	Androgen Receptor	Cancer
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC₅₀ of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC₅₀= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .

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

HY-N9917

Galloylalbiflorin 6′-O-Galloylalbiflorin	Paeonia lactiflora Pall. Source classification Polyphenols Plants Paeoniaceae	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-N2908

Atraric acid Methyl atrarate	Structural Classification Microorganisms Classification of Application Fields Phenols Essence, Fragrance Cosmetic Research Plants Inflammation/Immunology Disease Research Fields Cancer	Androgen Receptor NO Synthase p38 MAPK NF-κB
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-15758R

3,3'-Diindolylmethane (Standard)	Alkaloids Structural Classification other families Source classification Plants Alkaloid Dimers	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-N2908R

Atraric acid (Standard) Methyl atrarate (Standard)	Structural Classification Microorganisms Phenols Plants	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].

Cat. No.	Product Name	Chemical Structure

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[1][2][3].

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[1][2][3].

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[1].

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-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-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[1][2][3].

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[1].

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-16060S1

Apalutamide-d3
Apalutamide-d₃ is the deuterium labeled Apalutamide[1]. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[2].

HY-14249S1

Bicalutamide-d5
Bicalutamide-d₅ is deuterated labeled Bicalutamide (HY-14249). Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer .

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[1].

HY-16985S

Darolutamide-d4
Darolutamide-d₄ (ODM-201-d₄) is deuterium labeled Darolutamide. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC₅₀ of 26 nM in in vitro assay .

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-B1986S

p,p'-DDE-d8
p,p'-DDE-d₈ is the deuterium labeled p,p'-DDE[1]. 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 Ki of 3.5 μM[2].

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-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[1][2].

HY-111372S1

Finerenone-d5

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-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 .

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 the treatment 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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