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AR antagonist

" in MedChemExpress (MCE) Product Catalog:

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研究分野別:	Cancer (126) Cardiovascular Disease (50) Endocrinology (35) Infection (8) Inflammation/Immunology (46) Metabolic Disease (19) Neurological Disease (60)
クリックケミストリー:	PROTAC Synthesis (1)

271

阻害剤およびアゴニスト

蛍光色素

生化学アッセイ試薬

ペプチド

天然物

同位体標識化合物

クリックケミストリー

製品番号	製品名	Target	研究分野	構造式

HY-16985

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

HY-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-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-101106

AR7 10+ Cited Publications	RAR/RXR	Neurological Disease Cancer
AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy .

HY-A0295

(R)-Propranolol hydrochloride 1 Publications Verification	Adrenergic Receptor	Cardiovascular Disease Neurological Disease Endocrinology
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol (HY-B0573). 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 .

HY-110136

PMX 205 10+ Cited Publications	Complement System	Inflammation/Immunology
PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.

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-110136A

PMX 205 Trifluoroacetate 10+ Cited Publications	Complement System	Inflammation/Immunology
PMX 205 Trifluoroacetate is a specific complement *C5aR1* isoform antagonist .

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-19337

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

HY-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-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-136242

UT-34	Estrogen Receptor/ERR	Endocrinology Cancer
UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC₅₀ values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, *F876L-AR, and W741L-AR*, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.

HY-162412

PROTAC AR/AR-V7 degrader-1	PROTACs Adrenergic Receptor Apoptosis	Cancer
PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC₅₀ values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) .

HY-150102

EPI-7170 1 Publications Verification	Androgen Receptor	Cancer
EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .

HY-115282A

JNJ-63576253 1 Publications Verification TRC-253	Androgen Receptor	Cancer
JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC₅₀s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .

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-16985S

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

HY-136596

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

HY-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-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-16985R

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

HY-16060S

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

HY-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-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-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-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-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-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-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-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-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-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-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?(HY-B1208), or Histamine(HY-B1204)-induced contraction (β2) .

HY-149434

PROTAC AR-NTD degrader 1	Androgen Receptor PROTACs 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-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-108633

BYK 49187	PARP	Cancer
AR-C66096 (FPL 66096) tetrasodium is a selective platelet P2Y_T receptor antagonist. AR-C66096 tetrasodium effectively blocks ADP-induced platelet aggregation. AR-C66096 tetrasodium can be used in the research of thromboembolism .

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-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-148300

AR-C66096	P2Y Receptor	Cardiovascular Disease
AR-C66096 is a potent and selective antagonist of the Gi-coupled P2Y12 receptor. AR-C66096 suppresses platelet thrombus stability under physiological flow conditions. AR-C66096 inhibits ADP-induced aggregation in whole blood aggregometry. AR-C66096 can be used for antithrombotic research .

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-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-178148

*AR antagonist* 17**	Androgen Receptor	Endocrinology Cancer
AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC₅₀ = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC) .

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 .

製品番号	製品名	Target	研究分野

HY-106178

PMX-53 5+ Cited Publications 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-110136

PMX 205 10+ Cited Publications	Complement System	Inflammation/Immunology
PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.

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 .

HY-P5509

*C5aR1 antagonist* peptide**	ペプチド	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-P1345C

[DArg10, Aib20] TLQP-21	Drug Derivative Complement System	Neurological Disease Metabolic Disease Inflammation/Immunology
[DArg10, Aib20] TLQP-21, TLQP-21 (HY-P1345) analogue, is a C3aRpartial agonist, *C3aR* functional antagonist (EC₅₀: 854 nM for β-arrestin recruitment). [DArg10, Aib20] TLQP-21 shows no significant calcium flux activity. [DArg10, Aib20] TLQP-21 shows no activity in potentiating adrenergic-induced lipolysis. [DArg10, Aib20] TLQP-21 can be used in the research of inflammatory diseases, metabolic disorders, and neurological conditions .

製品番号	製品名	Category	Target	構造式

HY-B0573

Propranolol hydrochloride Maximum Cited Publications 44 Publications Verification	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Endocrinology Source Classification	Adrenergic Receptor Bacterial
Propranolol hydrochloride is a nonselective and BBB-permeableβ-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 44 Publications Verification	Cardiovascular Disease Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Source Classification	Adrenergic Receptor Bacterial
Propranolol is a nonselective and BBB-permeable 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-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-N2037

Higenamine 5+ Cited Publications Norcoclaurine; Demethyl-Coclaurine	Alkaloids Structural Classification Classification of Application Fields Ranunculaceae Phenols Polyphenols Aconitum carmichaeli Debx. Plants Isoquinoline Alkaloids Disease Research Fields Endocrinology Source Classification	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-N2908

Atraric acid Methyl atrARate	Structural Classification Microorganisms Classification of Application Fields Phenols Essence, Fragrance Cosmetic Research Plants Inflammation/Immunology Disease Research Fields Cancer	Environmental Pollutants NF-κB Androgen Receptor p38 MAPK NO Synthase
Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .

HY-N0475

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

HY-15758R

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

HY-B0573R

Propranolol hydrochloride (Standard)	Alkaloids Other Alkaloids Endogenous metabolite Source Classification	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-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-N2037R

Higenamine (Standard) Norcoclaurine (StandARd); Demethyl-Coclaurine (StandARd)	Alkaloids Structural Classification Ranunculaceae Phenols Polyphenols Aconitum carmichaeli Debx. Plants Isoquinoline Alkaloids Source Classification	Reference Standards 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-N0475R

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

HY-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].

製品番号	製品名	構造式

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-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-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-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-111372S

Finerenone-d3

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

HY-111372S1

Finerenone-d5

1 Publications Verification

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

HY-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-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-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-B1470S

Azaperone-d4

Azaperone-d₄ (R-1929-d₄) is the deuterium labeled Azaperone (HY-B1470). Azaperone is an antagonist of dopamine D2 receptor (Dopamine D2 Receptor) and α-adrenergic receptor (AR). Azaperone reduces vasomotor tone, mean arterial pressure, hematocrit, hemoglobin concentration, and etorphine-induced duration; induces transient tachycardia followed by bradycardia, splenic uptake of red blood cells, and sedation; alters animal behaviors; and produces sedation with distinct onset and duration in foals. Azaperone is used for sedation and tranquilization in various animals to reduce stress and aggressive behaviors, and serves as a preanesthetic agent.

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-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-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) .

HY-19337S1

Ketodarolutamide-d6

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

HY-19337S

Ketodarolutamide-d3

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

製品番号	製品名		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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