289 Results for "

AR antagonist

" in MedChemExpress (MCE) Product Catalog:
Products (289)

289 Results for "AR antagonist" in MCE Product Catalog:

246
246 Publications Verification
Cat. No.: HY-70002
CAS No.: 915087-33-1
Synonyms: MDV3100
Research Areas:  

Cancer

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .
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55
55 Cited Publications
Cat. No.: HY-B0573
CAS No.: 318-98-9
Propranolol hydrochloride is a nonselective and BBB-permeableβ-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki 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 .
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55
55 Cited Publications
Cat. No.: HY-B0573B
CAS No.: 525-66-6
Propranolol is a nonselective and BBB-permeable β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki 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 .
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52
52 Cited Publications
Cat. No.: HY-100543
CAS No.: 72795-26-7
Purity:  99.60%
Synonyms: ICI-118551
Zenidolol (ICI-118551) is a selective β2-adrenergic receptor antagonist with Ki values of Zenidolol for β2, β1 and β3 adrenergic receptors of 0.7, 49.5 and 611 nM, respectively. Zenidolol exerts antitumor effects via inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway by blocking β2-AR on tumor cells. Zenidolol exhibits a unique pulmonary vessel-specific vasodilatory effect in mouse models. Zenidolol can be used as an intraocular pressure-lowering agent in ophthalmic disease research .
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21
21 Cited Publications
Cat. No.: HY-14249
CAS No.: 90357-06-5
Purity:  99.91%
Research Areas:  

Cancer

Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer .
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18
18 Cited Publications
Cat. No.: HY-101106
CAS No.: 80306-38-3
Purity:  99.38%
Target:  

RAR/RXR

Research Areas:  

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 .
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17
17 Cited Publications
Cat. No.: HY-19532
CAS No.: 139180-30-6
Target:  

Adenosine Receptor

Research Areas:  

Neurological Disease Cancer

ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM .
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16
16 Cited Publications
Cat. No.: HY-16060
CAS No.: 956104-40-8
Synonyms: ARN-509
Target:  

Androgen Receptor

Research Areas:  

Cancer

Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
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16
16 Cited Publications
Cat. No.: HY-145388
CAS No.: 2380274-50-8
Purity:  99.89%
Target:  

PROTACs SWI/SNF Complex

Research Areas:  

Cancer

AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
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15
15 Cited Publications
Cat. No.: HY-110136
CAS No.: 514814-49-4
Purity:  99.54%
Target:  

Complement System

Research Areas:  

Inflammation/Immunology

PMX 205 is a potent complement C5a receptor (C5aR; CD88) antagonist.
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15
15 Cited Publications
Cat. No.: HY-110136A
Purity:  99.50%
Target:  

Complement System

Research Areas:  

Inflammation/Immunology

PMX 205 Trifluoroacetate is a specific complement C5aR1 isoform antagonist .
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13
13 Cited Publications
Cat. No.: HY-16985
CAS No.: 1297538-32-9
Synonyms: ODM-201; BAY-1841788
Target:  

Androgen Receptor

Research Areas:  

Cancer

Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki 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 .
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12
12 Cited Publications
Cat. No.: HY-15758
CAS No.: 1968-05-4
Purity:  99.89%
Synonyms: DIM; ARundine; HB 236
3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.
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12
12 Cited Publications
Cat. No.: HY-N2037
CAS No.: 5843-65-2
Synonyms: Norcoclaurine; Demethyl-Coclaurine
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 .
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11
11 Cited Publications
Cat. No.: HY-138161
CAS No.: 2411440-41-8
Purity:  99.59%
Target:  

Complement System

Research Areas:  

Inflammation/Immunology

JR14a is a potent thiophene antagonist of human complement C3a receptor. JR14a shows selectivity for the human C3a receptor over C5a receptor. JR14a can suppress C3aR-mediated inflammation .
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11
11 Cited Publications
Cat. No.: HY-111372
CAS No.: 1050477-31-0
Purity:  99.66%
Synonyms: BAY 94-8862
Finerenone (BAY 94-8862) is a third-generation, selective, and orally active 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 .
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9
9 Cited Publications
Cat. No.: HY-101978
CAS No.: 1202402-40-1
Purity:  99.85%
Synonyms: CPI-444; V81444
Target:  

Adenosine Receptor

Research Areas:  

Cancer

Ciforadenant (CPI-444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses .
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9
9 Cited Publications
Cat. No.: HY-106178
CAS No.: 219639-75-5
Purity:  99.98%
Synonyms: 3D53
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 .
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9
9 Cited Publications
Cat. No.: HY-129393
CAS No.: 2239273-34-6
Purity:  99.67%
Synonyms: AB928
Target:  

Adenosine Receptor

Research Areas:  

Inflammation/Immunology Cancer

Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities .
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5
5 Cited Publications
Cat. No.: HY-100186
CAS No.: 1539314-06-1
Purity:  99.74%
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 .
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