Search Result

Results for "

AR Antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5 alpha Reductase (1) 5-HT Receptor (14) Adenosine Receptor (47) Adrenergic Receptor (47) Androgen Receptor (80) Antibiotic (1) Apoptosis (6) Aryl Hydrocarbon Receptor (3) Autophagy (10) Bacterial (5) Calcium Channel (2) Carbonic Anhydrase (1) CD20 (1) Complement System (7) CXCR (1) Cytochrome P450 (2) Dopamine Receptor (1) Drug Metabolite (4) E3 Ligase Ligand-Linker Conjugates (1) Endogenous Metabolite (1) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (8) Formyl Peptide Receptor (FPR) (1) Fungal (3) Glucocorticoid Receptor (2) Imidazoline Receptor (1) Isotope-Labeled Compounds (13) Ligands for E3 Ligase (2) Ligands for Target Protein for PROTAC (5) mAChR (3) MAP3K (1) MDM-2/p53 (1) Mineralocorticoid Receptor (5) Neuropeptide Y Receptor (3) NF-κB (2) NO Synthase (2) Oxytocin Receptor (1) P2Y Receptor (3) p38 MAPK (2) PARP (1) Phosphodiesterase (PDE) (3) Progesterone Receptor (1) Prostaglandin Receptor (1) PROTACs (3) RAR/RXR (1) Reactive Oxygen Species (ROS) (2) Reference Standards (16) Renin (3) ROS Kinase (1) Ser/Thr Protease (1) Vasopressin Receptor (1)
By Research Areas:	Cancer (99) Cardiovascular Disease (39) Endocrinology (32) Infection (5) Inflammation/Immunology (35) Metabolic Disease (10) Neurological Disease (46)
Click Chemistry:	PROTAC Synthesis (1)

222

Inhibitors & Agonists

Fluorescent Dye

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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 .

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-173409

*AR antagonist* 11**	Androgen Receptor Ser/Thr Protease	Inflammation/Immunology
AR antagonist 11 (Compound c2) is a selective AR antagonist with an IC₅₀ of 0.019 μM. AR antagonist 11 is also effective against AR ^F877L/T878A mutant (IC₅₀: 1.03 μM). AR antagonist 11 inhibits LNCaP cell proliferation and reduces PSA protein expression (IC₅₀: 0.54 μM). AR antagonist 11 can be used for research of prostate cancer (PCa) .

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-173559

*AR antagonist* 12**	Androgen Receptor	Cancer
AR antagonist 12 (compound 20i) is an orally active androgen receptor antagonist wiith IC₅₀ values of 119.3 μM and 98.2 μM for wt-AR and AR-F877L,respectively. AR antagonist 12 induces a dose-dependent and time-dependent reduction in AR, AR-V7, and PSA protein levels. AR antagonist 1 shows anticancer activuty and can be used for the study of Enzalutamide (HY-70002)-resistant 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-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-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-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-159922

*AR antagonist* 9**	Androgen Receptor	Cancer
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC₅₀ value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC₅₀ = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against AR_F876L/T877A and AR_W741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .

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-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-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-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-172624

*AR antagonist* 14**	Ligands for Target Protein for PROTAC	Cancer
AR antagonist 14 is is a PROTAC target protein ligand (Ligands for Target Protein for PROTAC). AR antagonist 14 can be combined with VH 101-amide-piperidine-Pip-alkyne (HY-172625) to synthesize PROTAC degraders (ARD-69 (HY-114402)) .

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-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-136960

*β2AR antagonist* 1**	Adrenergic Receptor	Others
β2AR antagonist 1 (Cmpd-15PA) is an antagonist of β2 adrenergic receptor (β2AR). β2AR antagonist 1 binds to the intracellular surface of the β2AR .

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-163378

*C5aR1 antagonist* 1**	Complement System	Inflammation/Immunology
C5aR1 antagonist 1 (Compound 7e) is an orally active C5a receptor 1 (C5aR1) antagonist. C5aR1 antagonist 1 is active in DISCO and migration assays, with IC₅₀ values of 38 nM and 17 nM, respectively. C5aR1 antagonist 1 can be used for the research of acute and chronic inflammatory diseases .

HY-144115

*A1AR antagonist* 1**	Adenosine Receptor	Neurological Disease
A1AR antagonist 1 (compound 18g) is a potent A₁ adenosine receptor (AR) antagonist with K_is of 2.08, 6.91, and 31.2 nM for hA1, hA2A and hA2B, respectively .

HY-147544

*A1AR antagonist* 5**	Adenosine Receptor	Neurological Disease
A1AR antagonist 5 (compound 20) is a potent and selective *A1AR* (A1 adenosine receptor) antagonist, with a pIC₅₀ of 5.83 and a pK_i of 6.11 .

HY-147543

*A1AR antagonist* 4**	Adenosine Receptor	Neurological Disease
A1AR antagonist 4 (compound 22) is a potent and selective *A1AR* (A1 adenosine receptor) antagonist, with a pIC₅₀ of 5.51 and a pK_i of 6.29 .

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-163379

*C5aR1 antagonist* 2**	Complement System	Inflammation/Immunology
C5aR1 antagonist 2 (Compound 6a) is an orally active C5a receptor 1 (C5aR1) antagonist that shows efficacy in inhibiting the C5a-induced neutrophil count increase. C5aR1 antagonist 2 is potent in the DISCO and migration assays, with IC₅₀ values of 21 and 3 nM, respectively. C5aR1 antagonist 2 can be used for the research of acute and chronic inflammatory diseases .

HY-163363

*β-AR antagonist* 2**	Adrenergic Receptor	Cancer
β-AR antagonist 2 (compound 43) is an antagonist of *β-AR* (IC₅₀: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice .

HY-146456

*A1AR antagonist* 3**	Adenosine Receptor	Neurological Disease
A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with K_is of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases .

HY-144116

*A1AR antagonist* 2**	Adenosine Receptor	Neurological Disease
A1AR antagonist 2 (compound 18h) is a potent A₁ adenosine receptor (AR) antagonist with K_is of 1.49, 10.2, and 50.1 nM for hA₁, hA_2A and hA_2B, respectively .

HY-W471937

*α1B-AR antagonist* 1**	Adrenergic Receptor	Cardiovascular Disease Neurological Disease
α1b-AR antagonist 1 (Compound Cpd1) is a selective *α₁B-AR* antagonist. Alpha1b-ar antagonist 1 can be used in the study of cardiovascular and central nervous system diseases .

HY-12099

*A3AR antagonist* 2**	Adenosine Receptor	Inflammation/Immunology
A3AR antagonist 2 (compound 18) is a potent Human A3 adenosine receptor antagonist with an K_i value of 4.54 nM .

HY-164621

*A3AR antagonist* 5**	Adenosine Receptor	Others
A3AR antagonist 5 (Compound 16) is a selective antagonist for human adenosine A3 receptor with an affinity pC of 4.542 μM .

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-158057

*A2AR/A2BR antagonist* 1**	Adenosine Receptor	Cancer
A_2AR/A_2BR antagonist 1 (compound 7ai) has a dual antagonistic effect on *A_2AR/A_2BR, with the IC₅₀* values of 11.2 nM and 6.4 nM for *A_2AR* and A_2BR, respectively. A_2AR/A_2BR antagonist 1 promotes T cell-mediated cancer cell death .

HY-145862

*5-HT6/5-HT2AR antagonist-1*	5-HT Receptor	Neurological Disease
5-HT6/5-HT2AR antagonist-1 is a potent dual *5-HT₆/5-HT_2AR* antagonist with K_i values of 11 nM and 39 nM, respectively .

HY-153333

*A1/A3 AR antagonist* 3**	Adenosine Receptor	Cardiovascular Disease
A1/A3 AR antagonist 3 is an A₁R/A₃R dual antagonist with high affinity at low-micromolar to low-nanomolar. A1/A3 AR antagonist 3 can be used for the research of chronic heart diseases .

HY-145706

*A2A/A1 AR antagonist-1*	Adenosine Receptor	Neurological Disease
A2A/A1 AR antagonist-1 (compound 1a) is dual potent A_2A/A₁ AR antagonist with K_is of 5.58 and 24.2 nM, respectively. A2A/A1 AR antagonist-1 has the potential for the research of ischemic stroke .

HY-147541

*A2A/A3 AR antagonist-1*	Adenosine Receptor	Inflammation/Immunology
A2A/A3 AR antagonist-1 (compound 23) is a dual A_2A/A₃ adenosine receptor (AR) fluorescent ligand, with K_is of 90 nM and 31.8 nM for hA_2A AR and hA₃ AR, respectively .

HY-146478

*A1/A3 AR antagonist* 1**	Adenosine Receptor	Neurological Disease Inflammation/Immunology
A1/A3 AR antagonist 1 (compound 10) is a potent adenosine 1 (A1) and adenosine 3 (A3) receptor dual antagonist with K_is of 36.7 nM, 25.4 nM and 1.47 nM for human A1, human A3 and rat A1, respectively. A1/A3 AR antagonist 1 can be used for researching kidney failure, inflammatory pulmonary diseases, and Alzheimer’s disease .

HY-148533

*β2AR agonist* /M-receptor antagonist-1**	mAChR Adrenergic Receptor	Neurological Disease
β2AR agonist /M-receptor antagonist-1 is a potent dual *muscarinic antagonist/beta 2 agonist* (MABA)*. β2AR agonist* /M-receptor antagonist-1 potently relaxes either Carbachol (HY-B1208)-induced contraction, in the absence (MABA) or presence of Propranolol (M3; HY-B1208), or Histamine (HY-B1204)-induced contraction (β2) .

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-146479

*A1/A3 AR antagonist* 2**	Adenosine Receptor	Inflammation/Immunology
The compound is an a1/a3 adenosine receptor antagonist, which helps to research (neurological) inflammatory diseases.

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-149434

PROTAC AR-NTD degrader 1	Androgen Receptor Apoptosis	Cancer
PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively .

HY-106769B

(3aR,9aR)-Fluparoxan (3AR,9AR)-GR50360	Adrenergic Receptor	Neurological Disease
(3aR,9aR)-Fluparoxan ((3aR,9aR)-GR50360) is a highly selective and potent α2B adrenaline receptor antagonist with the activity of preventing, improving or inhibiting neurodevelopmental disorders and neurodegenerative diseases. As an α2B receptor antagonist, (3aR,9aR)-Fluparoxan can promote the recovery of neurological function. The mechanism of action of (3aR,9aR)-Fluparoxan makes it have important application potential in neuroscience research .

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-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-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-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-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 .

Cat. No.	Product Name	Type

HY-D1606

BODIPY FL prazosin	Fluorescent Dyes/Probes
BODIPY FL prazosin is a fluorescent α1-adrenergic antagonist with K_i values of 14.5, 43.3 nM for α1a-AR and α1b-AR, respectively. BODIPY FL prazosin also is a fluorescent ligand with the excitation and emission wavelengths are 485 and 535 nm, respectively. BODIPY FL prazosin can be used for study the differences in the subcellular localization of α1-adrenoceptor subtypes .

Cat. No.	Product Name	Target	Research Area

HY-110136

PMX 205 5+ Cited Publications	Complement System	Inflammation/Immunology
PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.

HY-106178

PMX-53 4 Publications Verification 3D53	Complement System	Cardiovascular Disease Inflammation/Immunology Cancer
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC₅₀ of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to *C5aR1* and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects .

HY-P5509

*C5aR1 antagonist* peptide**	Peptides	Others
C5aR1 antagonist peptide is a biological active peptide. (This linear peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions to inhibit C5a binding and function at human and rat C5a receptors. C5a is crucial to triggering cellular immune responses and its overexpression is involved in arthritis, Alzheimer’s disease, cystic fibrosis, systemic lupus erythematosus, and other immunoinflammatory diseases.)

HY-P5010

(D-Arg8)-Inotocin	Vasopressin Receptor	Cardiovascular Disease
(D-Arg8)-Inotocin is a potent, selective and competitive antagonist of vasopressin receptor (V_1aR), with a K_i of 1.3 nM. (D-Arg8)-Inotocin shows more than 3000-fold selectivity for the human V1aR over the other three subtypes, OTR, V1bR and V2R .

Cat. No.	Product Name	Target	Research Area

HY-P99483

Blontuvetmab AT 004; VT 007	CD20 Adenosine Receptor	Cancer
Blontuvetmab (AT 004) is a caninized CD20 monoclonal antibody and is also a potent, selective, highly potent antagonist of A2aR receptor. Blontuvetmab behaves as Nociceptin (HY-P0183)/Orphanin (HY-P0183) FQ receptor (NOP) agonists displaying weak NOP affinity. Blontuvetmab inhibits 5'-N-Ethylcarboxamidoadenosine (NECA)-mediated A2aR activation and significantly reverses the ability of adenosine to suppress CD8 T cell activation, increasing levels of cytokines such as IFN-γ. Blontuvetmab Blontuvetmab can be used for the research of Canine B-cell lymphoma .

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-B0573

Propranolol hydrochloride Maximum Cited Publications 31 Publications Verification	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields Endocrinology	Adrenergic Receptor Bacterial
Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0573B

Propranolol Maximum Cited Publications 31 Publications Verification	Cardiovascular Disease Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields	Adrenergic Receptor Bacterial
Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

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-N2037

Higenamine 4 Publications Verification Norcoclaurine; Demethyl-Coclaurine	Alkaloids Structural Classification Classification of Application Fields Ranunculaceae Source classification Phenols Polyphenols Aconitum carmichaeli Debx. Plants Isoquinoline Alkaloids Disease Research Fields Endocrinology	MAP3K MDM-2/p53 Adrenergic Receptor ROS Kinase Apoptosis
Higenamine (Norcoclaurine), a *β2-AR* agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC₅₀=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .

HY-15758R

3,3'-Diindolylmethane (Standard) DIM (StandARd); ARundine (StandARd); HB 236 (StandARd)	Alkaloids Structural Classification other families Source classification Plants Alkaloid Dimers	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-W008226R

Phloracetophenone (Standard) 2,4,6-trihydroxyacetophenone (StandARd); 1-(2,4,6-Trihydroxyphenyl)ethanone (StandARd)	Structural Classification other families Ketones, Aldehydes, Acids Source classification Phenols Polyphenols Plants 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-B0573R

Propranolol hydrochloride (Standard)	Alkaloids Other Alkaloids Source classification Endogenous metabolite	Reference Standards Adrenergic Receptor Bacterial
Propranolol (hydrochloride) (Standard) is the analytical standard of Propranolol (hydrochloride). This product is intended for research and analytical applications. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-N2908R

Atraric acid (Standard) Methyl atrARate (StandARd)	Structural Classification 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-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-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-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-12715S

Yohimbine-13C,d3
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-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-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-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-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-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-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-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-B0573BS

Propranolol-d7

Propranolol-d₇ is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0573S

Propranolol-d7 hydrochloride

Propranolol-d₇ (hydrochloride) is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

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-B0573S1

Propranolol-d7 (ring-d7)

Propranolol-d₇ (ring-d₇) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-W742404

Bopindolol-d9

Bopindolol-d₉ ((±)-Bopindolol-d₉) is the deuterium labeled Bopindolol (HY-B1562). Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.

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-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-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

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-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 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).

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks