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AR+antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Adenosine Receptor (42) Adrenergic Receptor (20) Androgen Receptor (69) Antibiotic (1) Apoptosis (2) Arrestin (2) Aryl Hydrocarbon Receptor (3) Autophagy (9) Bacterial (2) Calcium Channel (2) Complement System (1) COX (1) Cytochrome P450 (2) Drug Intermediate (1) Drug Metabolite (3) Endogenous Metabolite (1) Environmental Pollutants (3) Estrogen Receptor/ERR (6) Fungal (3) GABA Receptor (1) HDAC (1) Herbicide (1) IKK (1) Interleukin Related (1) Isotope-Labeled Compounds (11) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (4) NF-κB (3) NO Synthase (3) p38 MAPK (2) Phosphodiesterase (PDE) (3) PROTACs (3) Reactive Oxygen Species (ROS) (3) Reference Standards (18) Ser/Thr Protease (1) SWI/SNF Complex (1) TNF Receptor (1)
By Research Areas:	Cancer (82) Cardiovascular Disease (14) Endocrinology (18) Infection (6) Inflammation/Immunology (22) Metabolic Disease (8) Neurological Disease (23)
Click Chemistry:	PROTAC Synthesis (1)

148

Inhibitors & Agonists

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Isotope-Labeled Compounds

Click Chemistry

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-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-19532

ZM241385 10+ Cited Publications	Adenosine Receptor	Neurological Disease Cancer
ZM241385 is a potent, high affinity and selective adenosine A_2a receptor (A_2AR) antagonist with a K_i value of 1.4 nM .

HY-101978

Ciforadenant 5+ Cited Publications CPI-444; V81444	Adenosine Receptor	Cancer
Ciforadenant (CPI-444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses .

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-17497A

Acebutolol hydrochloride 3 Publications Verification	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Acebutolol hydrochloride is an orally active β1 adrenergic receptor (β1AR) antagonist. Acebutolol hydrochloride is used in the treatment of hypertension, angina pectoris and cardiac arrhythmias .

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-101980

Imaradenant 3 Publications Verification HTL1071; AZD4635	Adenosine Receptor	Cancer
AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a K_i of 1.7 nM and shows >30-fold selectivity over other adenosine receptors .

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-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-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-B1486

Oxprenolol hydrochloride 1 Publications Verification Ba 39089	Adrenergic Receptor	Cardiovascular Disease
Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

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-153152

DPTN dihydrochloride	Adenosine Receptor	Inflammation/Immunology
DPTN is a potent and selective human, mouse, and rat A ³AR antagonist with K_i values of 1.65, 9.61, and 8.53 nM, respectively .

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-17497

Acebutolol 3 Publications Verification	Adrenergic Receptor	Cardiovascular Disease
Acebutolol is an orally active β1 adrenergic receptor (β1AR) antagonist. Acebutolol is used for hypertension, angina pectoris and cardiac arrhythmias research .

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-103162

ANR94	Adenosine Receptor	Neurological Disease
ANR94 is a potent and selective adenosine A_2A receptor (AA_2AR) antagonist with an K_i of 46 nM for hAA_2AR. ANR94 has the potential for the research of Parkinson's disease .

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-103190

MRS1220	Adenosine Receptor	Neurological Disease Cancer
MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a K_i of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system . MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo .

HY-149916

A2AR-antagonist-1	Adenosine Receptor	Cancer
A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC₅₀=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t_1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) .

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-W007367

2,6-Dichloropurine	Drug Intermediate	Others
2,6-Dichloropurine is a pharmaceutical intermediate. 2,6-Dichloropurine can be used to synthesize various PDE inhibitors, human A3 adenosine receptor (AR) antagonists, and CDK inhibitors .

HY-15996

Seviteronel VT-464	Cytochrome P450 Androgen Receptor	Cancer
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC₅₀=69 nM) and an AR antagonist. Seviteronel demonstrates both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.

HY-136960

β2AR antagonist 1	Adrenergic Receptor	Others
β2AR antagonist 1 is a potent β2-adrenergic receptor (β2AR) inhibitor. β2AR antagonist 1 exhibits high selectivity for β2AR over β1AR, vasopressin receptor type 2, and angiotensin type 1 receptor. β2AR antagonist 1 stabilizes the inactive conformation of β2AR and interferes with its coupling to G proteins and β-arrestins .

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-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-134555

A3AR antagonist 4	Adenosine Receptor	Neurological Disease
A3AR antagonist 4 (Compd 1) is an *A3AR* antagonist, with K_i values of 30.8 nM (hA₃) and 203 nM (hA₁), repectively. A3AR antagonist 4 (Compd 1) can be used for the study of cerebral ischemia .

HY-147545

A1AR antagonist 6	Adenosine Receptor	Neurological Disease
A1AR antagonist 6 (compound 15) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC₅₀ of 6.38 and a pK_i of 7.13 .

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-B1486AS

Oxprenolol-d7	Isotope-Labeled Compounds Adrenergic Receptor	Cardiovascular Disease
Oxprenolol-d₇ is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

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-174391

AR antagonist 15	Androgen Receptor Apoptosis	Cancer
AR antagonist 15 is an orally active androgen receptor (AR) antagonist with the IC₅₀ of 97 nM for AR^T787A. AR antagonist 15 disrupts AR nuclear translocation, hinders AR homodimerization, and suppresses transcription of AR-regulated genes by competitive binding to the ligand binding pocket. AR antagonist 15 can significantly lower the prostate-specific antigen (PSA) level. AR antagonist 15 induces apoptosis by reducing the expression of apoptosis pathway related proteins. AR antagonist 15 can be used for the research of prostate cancer.

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 .

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-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-146457

A3AR antagonist 1	Adenosine Receptor	Inflammation/Immunology
A3AR antagonist 1 (compound 17) is a potent and selective human A₃ adenosine receptor (AR) antagonist, with an K_i of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A₃ AR even at high concentrations .

HY-120652

A3AR antagonist 3	Adenosine Receptor	Inflammation/Immunology
A3AR antagonist 3 (compound 21) is a selective A3 adenosine receptor (A3AR) antagonist with a K_i of 37 nM. A3AR antagonist 3 shows >60-fold selectivity in comparison to A1 and A2A adenosine receptors .

HY-119170

BMS-779333	Androgen Receptor	Neurological Disease Cancer
BMS-779333 is an orally active androgen receptor (AR) antagonist. BMS-779333 is promising for research of prostate cancer and seizure .

HY-14249S

Bicalutamide-d4	Isotope-Labeled Compounds Androgen Receptor Autophagy	Cancer
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-B1486A

Oxprenolol Ba 39089 free base	Adrenergic Receptor	Cardiovascular Disease
Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-16060R

Apalutamide (Standard) ARN-509 (Standard)	Reference Standards Androgen Receptor	Cancer
Apalutamide (Standard) is the analytical standard of Apalutamide. This product is intended for research and analytical applications. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM .

HY-16060S3

Apalutamide-d7 ARN-509-d₇	Androgen Receptor Isotope-Labeled Compounds	Cancer
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-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-16060S2

Apalutamide-13C,d3 ARN-509-¹³C,d₃	Isotope-Labeled Compounds Androgen Receptor	Cancer
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-B1486S

Oxprenolol-d7 hydrochloride Ba 39089-d₇	Adrenergic Receptor	Cardiovascular Disease
Oxprenolol-d₇ (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-19532R

ZM241385 (Standard)	Adenosine Receptor	Neurological Disease Cancer
ZM241385 (Standard) is the analytical standard of ZM241385. This product is intended for research and analytical applications. ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM .

HY-170951

AR antagonist 10	Androgen Receptor	Cancer
AR antagonist 10 (Compound Y5) is potent and orally active androgen receptor (AR) antagonist with an IC₅₀ of 0.04 μM. AR antagonist 10 demonstrates dual mechanisms of action, antagonizes AR by disrupting AR dimerization, and induces AR degradation via the ubiquitin-proteasome pathway. AR antagonist 10 exhibits excellent activity against variant drug-resistant AR mutants. AR antagonist 10 effectively suppresses the tumor growth of the LNCaP xenograft. AR antagonist 10 is potential to be used for drug-resistant prostate cancer .

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-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-W008226R

Phloracetophenone (Standard) 2,4,6-trihydroxyacetophenone (Standard); 1-(2,4,6-Trihydroxyphenyl)ethanone (Standard)	Structural Classification other families Ketones, Aldehydes, Acids Phenols Polyphenols Plants Source Classification Curcuma comosa Roxb. Zingiberaceae	Reference Standards Cytochrome P450 Bacterial Antibiotic
Oxprenolol (hydrochloride) (Standard) is the analytical standard of Oxprenolol (hydrochloride). This product is intended for research and analytical applications. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle .

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].

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-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-B1486AS

Oxprenolol-d7
Oxprenolol-d₇ is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

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-B1486S

Oxprenolol-d7 hydrochloride
Oxprenolol-d₇ (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle .

HY-12715S

Yohimbine-13C,d3 1 Publications Verification
Yohimbine- ¹³C,d₃ is the ¹³C- and deuterium labeled Yohimbine. Yohimbine is a potent and relatively nonselective alpha 2-adrenergic receptor (AR) antagonist, with IC50 of 0.6 μM.

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-19532S

ZM241385-d7
ZM241385-d7 is a deuterated form of ZM241385 (HY-19532). ZM241385 is a potent, high affinity and selective adenosine A_2a receptor (A_2AR) antagonist with a K_i value of 1.4 nM .

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-166478S

O-Desmethyl carvedilol-d5

O-Desmethyl carvedilol-d₅ (Desmethylcarvedilol-d₅) is deuterium labeled O-Desmethylcarvedilol. O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of the non-selective β-adrenergic receptor (β-AR) antagonist Carvedilol (HY-B0006). O-Desmethylcarvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2 ^R4496C) mutation (IC₅₀ = 7.62 μM). O-Desmethylcarvedilol reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by Isoproterenol (HY-B0468) in conscious rabbits (ED₅₀s = 32 and 5 μg/kg, respectively) .

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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