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adenosine A3 receptor antagonist

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By Targets:	Adenosine Receptor (45) Androgen Receptor (1) Apoptosis (1) Biochemical Assay Reagents (2) Calcium Channel (2) Drug Intermediate (1) p38 MAPK (1) PGC-1α (1) Phosphodiesterase (PDE) (1) PI3K (2) Platelet-activating Factor Receptor (PAFR) (1) Reference Standards (5)
By Research Areas:	Cancer (14) Cardiovascular Disease (7) Inflammation/Immunology (24) Metabolic Disease (3) Neurological Disease (11)

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Biochemical Assay Reagents

Natural
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Targets Recommended: Adenosine Kinase Adenosine Deaminase Adenosine Receptor

Cat. No.	상품명	Target	연구분야	Chemical Structure

HY-19533

SCH 58261 Maximum Cited Publications 17 Publications Verification	Adenosine Receptor	Cancer
SCH 58261 is a potent, selective and competitive antagonist of **adenosine A2A receptor with an IC₅₀** of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively .

HY-14121

MRS 1754 5+ Cited Publications	Adenosine Receptor	Metabolic Disease Inflammation/Immunology
MRS 1754 is a selective antagonist radioligand for A_2B adenosine receptor with very low affinity for A₁ and A₃ receptors of both humans and rats .

HY-100678

CGS 15943	Adenosine Receptor PI3K	Inflammation/Immunology Cancer
CGS 15943 is an orally bioavailable non-xanthine **Adenosine Receptor** antagonist. Its K_i for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .

HY-121119

MRS 1523 5 Publications Verification	Adenosine Receptor Calcium Channel	Cardiovascular Disease Neurological Disease Inflammation/Immunology
MRS 1523 is a potent and selective **adenosine A₃ receptor** antagonist with K_i values of 18.9 nM and 113 nM for human and rat A₃ receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A₁ and A_2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons .

HY-103166

PSB-603 3 Publications Verification	Adenosine Receptor	Inflammation/Immunology
PSB-603 is a potent and highly selective A_2B adenosine receptor antagonist exhibiting a K_i value of 0.553 nM and virtually no affinity for the human and rat A₁ and A_2A and the human A₃ receptors up to a concentration of 10 μM .

HY-14858

Derenofylline 2 Publications Verification SLV 320	Adenosine Receptor	Cardiovascular Disease
Derenofylline (SLV 320) is a potent, selective and orally active **adenosine A₁ receptor** antagonist, with K_i values of 1 nM, 200 nM and 398 nM for human A₁, A₃ and A_2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats .

HY-119413

9-Ethyladenine	Adenosine Receptor	Neurological Disease
9-Ethyladenine is a precursor of competitive antagonists of **adenosine receptors** (A₁, A₂, A₃), with no significant inhibitory effect on adenine phosphoribosyltransferase (APRT). 9-Ethyladenine derivatives have high affinity and selectivity for A₁ (K_i=27 nM), A₂A (K_i=46 nM), and A₃ (K_i=86 nM) receptors. 9-Ethyladenine does not inhibit brain APRT activity, can be used in the study of adenosine receptor-related diseases (such as nervous system diseases) models .

HY-124543

MRS-1191 4 Publications Verification	Adenosine Receptor	Neurological Disease
MRS-1191 is a potent and selective A₃ adenosine receptor antagonist with a K_B value of 92 nM, a K_i value of 31.4 nM for human A₃ receptor and an IC₅₀ of 120 nM for CHO cells . MRS-1191 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-148088

M1069 1 Publications Verification	Adenosine Receptor	Cancer
M1069 is a selective and orall active, dual A_2A/A_2B adenosine receptor antagonist with a selectivity of >100 fold against the A₁ and A₃ receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity .

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-103174

MRS1334	Adenosine Receptor	Cardiovascular Disease
MRS1334 is a potent and selective human **adenosine A₃ receptor** antagonist with K_is of 2.69 nM, >100 nM, >100 nM for hA₃, rA₁, rA_2A, respectively. MRS1334 blocks the protective effect of Cl-IB-MECA leading to significant bradycardia and elevated ST segment . MRS1334 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-110037

MRS-3777 hemioxalate	Adenosine Receptor	Neurological Disease
MRS-3777 hemioxalate is a selective **adenosine A3 receptor** antagonist .

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-111767

BAY-545	Adenosine Receptor	Inflammation/Immunology
BAY-545 is a potent and selective A_2B adenosine receptor antagonist, with an IC₅₀ of 59 nM. BAY-545 also exhibits IC₅₀s of 66, 400, 280 nM for human, mouse, rat A_2B adenosine receptor in cells, respectively, and a K_i of 97 nM for human A_2B adenosine receptor, with more selectivity over A₁, A_2A, and A₃ adenosine receptor .

HY-107497

1-Methyl-3-amino-4-cyanopyrazole	Biochemical Assay Reagents	Cancer
1-Methyl-3-amino-4-cyanopyrazole (compound 3) is a molecular compound that can be used in the synthesis of adenosine A3 receptor antagonists. 1-Methyl-3-amino-4-cyanopyrazole can be utilized in cancer research .

HY-103178

MRE3008F20	Adenosine Receptor	Inflammation/Immunology
MRE3008F20 is a highly efficient, highly selective and radioactive **adenosine A₃ receptor (AA₃R*) antagonist* (K_i=1.8 nM). MRE3008F20 effectively antagonises Cl-IB-MECA-induced cAMP production in resting lymphocytes with an IC₅₀ value of 5 nM. MRE3008F20 can be used in the study of AA3R .

HY-103176

PSB11 hydrochloride	Adenosine Receptor	Others
PSB11 hydrochloride is an antagonist with reverse excitatory activity for human A3 **Adenosine Receptor** with high affinity (K_i=2.3 nM) .

HY-100274

Adenosine antagonist-1	Adenosine Receptor	Inflammation/Immunology
Adenosine antagonist-1 is an **adenosine A3 receptor (AA3R*) antagonist* with anti-inflammatory activity.

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-148076

A2A receptor antagonist 3	Adenosine Receptor	Cancer
A2A receptor antagonist 3 (Example 92) is an **adenosine A2a receptor** antagonist with a K_i of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with K_is of 37, 107 and 1467 nM, respectively .

HY-103177

PSB-10 hydrochloride	Adenosine Receptor	Inflammation/Immunology
PSB-10 hydrochloride is a potent and selective antagonist of *human adenosine* A3 receptor (A₃AR), with a K_i** of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA₃ over rA₁, rA_2A, hA₁, hA_2A and hA_2B receptors (K_i=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice .

HY-103167

CGH2466 dihydrochloride	Adenosine Receptor p38 MAPK Phosphodiesterase (PDE)	Inflammation/Immunology
CGH 2466 dihydrochloride is an orally active **adenosine A1, A2B and A3 receptor** antagonist with the IC₅₀ values of 19 nM, 21 nM, and 80 nM respectively. CGH 2466 dihydrochloride inhibits p38 MAPK (IC₅₀ = 187~ 400 nM) and phosphodiesterase type 4D (IC₅₀ = 22 nM). CGH 2466 dihydrochloride displays potent anti-inflammatory effects both in vitro and in vivo, and can be used for research on asthma and chronic obstructive pulmonary disease (COPD) .

HY-118086

MRS1067	Adenosine Receptor	Inflammation/Immunology Cancer
MRS 1067 is a competitive antagonist of the **adenosine A3 receptor that inhibits the suppression of adenylate cyclase** by adenosine A3 receptor agonists and affects the activation of G proteins. MRS 1067 can be used in research related to inflammation and cancer .

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-120090

MRS1177	Adenosine Receptor	Inflammation/Immunology
MRS1177 is a potent and selective human Adenosine A3 receptor (hA₃AR) antagonist, with a K_i of 0.3 nM.

HY-118678

MRS1186	Adenosine Receptor	Inflammation/Immunology
MRS1186 is a potent and selective human Adenosine A3 receptor (hA₃AR) antagonist, with a K_i of 7.66 nM.

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-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-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-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-119191

KF26777 free base	Adenosine Receptor	Neurological Disease
KF26777 (free base) is a potent and selective **adenosine A3 receptor** antagonist with an K_i value of 0.2 nM and possesses 9000-, 2350- and 3100-fold selectivity against adenosine A1, A2A and A2B receptors, respectively. KF26777 (free base) potently inhibits the [125I]AB-MECA binding to **adenosine A3 receptors**. KF26777 (free base) is promising for research of brain ischemia and inflammatory disease including asthma .

HY-162787

Adenosine receptor antagonist 5	Adenosine Receptor	Cancer
Adenosine receptor antagonist 5 (Compound 39) is a selective antagonist for *human adenosine* A3 receptor (hA3R) with K_i** of 12 nM. Adenosine receptor antagonist 5 inhibits IB-MECA (HY-13591)-induced cAMP accumulation in NCI-H1792 cell, inhibits the proliferation of cancer cell LK-2 and NCI-H1792. Adenosine receptor antagonist 5 exhibits a fast metabolic rate in human liver microsomes .

HY-14121R

MRS 1754 (Standard)	Adenosine Receptor	Metabolic Disease Inflammation/Immunology
MRS 1754 (Standard) is the analytical standard of MRS 1754. This product is intended for research and analytical applications. MRS 1754 is a selective antagonist radioligand for A2B adenosine receptor with very low affinity for A1 and A3 receptors of both humans and rats .

HY-148088A

M1069 free base 1 Publications Verification	Adenosine Receptor	Cancer
M1069 (free base) is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 (free base) counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity .

HY-124543R

MRS-1191 (Standard)	Adenosine Receptor	Neurological Disease
MRS-1191 (Standard) is the analytical standard of MRS-1191. This product is intended for research and analytical applications. MRS-1191 is a potent and selective A3 adenosine receptor antagonist with a KB value of 92 nM, a Ki value of 31.4 nM for human A3 receptor and an IC50 of 120 nM for CHO cells . MRS-1191 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-100678R

CGS 15943 (Standard)	Reference Standards Adenosine Receptor PI3K	Inflammation/Immunology Cancer
CGS 15943 (Standard) is the analytical standard of CGS 15943. This product is intended for research and analytical applications. CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .

HY-121119R

MRS 1523 (Standard)	Adenosine Receptor Calcium Channel	Cardiovascular Disease Neurological Disease Inflammation/Immunology
MRS 1523 (Standard) is the analytical standard of MRS 1523. This product is intended for research and analytical applications. MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons .

HY-123038

CVT-5440	Adenosine Receptor	Inflammation/Immunology
CVT-5440 is a xanthine based, selective, high affinity *A_2B adenosine* receptors (AdoR)** antagonist with a K_i of 50 nM (selectivity A₁> 200; A_2A>200; A₃>167). CVT-5440 has the potential for asthma research .

HY-19533R

SCH 58261 (Standard)	Adenosine Receptor	Cancer
SCH 58261 (Standard) is the analytical standard of SCH 58261. This product is intended for research and analytical applications. SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively .

HY-14858R

Derenofylline (Standard) SLV 320 (Standard)	Adenosine Receptor Reference Standards	Cardiovascular Disease
Derenofylline (Standard) is the analytical standard of Derenofylline. This product is intended for research and analytical applications. Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats .

HY-107497R

1-Methyl-3-amino-4-cyanopyrazole (Standard)	Reference Standards Biochemical Assay Reagents	Cancer
1-Methyl-3-amino-4-cyanopyrazole (Standard) is the analytical standard of 1-Methyl-3-amino-4-cyanopyrazole (HY-107497). This product is intended for research and analytical applications. 1-Methyl-3-amino-4-cyanopyrazole (compound 3) is a molecular compound that can be used in the synthesis of adenosine A3 receptor antagonists. 1-Methyl-3-amino-4-cyanopyrazole can be utilized in cancer research .

HY-118232

VUF8504	Adenosine Receptor	Cardiovascular Disease
VUF-8504 is a potent and selective **adenosine A3 receptor** antagonist with K_i value of 0.017, 14 nM for human A3, A1, respectively .

HY-182432

A3AR antagonist-7	Adenosine Receptor	Cancer
A3AR antagonist-7 is a conjugable human A3 adenosine receptor (A3AR) antagonist with a K_i value of 31.8 nM. A3AR antagonist-7 is applicable to the research of melanoma, breast cancer and colorectal cancer .

HY-182583

PAF antagonist-1	Platelet-activating Factor Receptor (PAFR)	Cardiovascular Disease
PAF antagonist-1 is a platelet activating factor (PAF) *receptor* antagonist with a target K_i of 69 nM. PAF antagonist-1 inhibits PAF binding and displays enhanced affinity at A₁, A₂ ^a, and A₃ adenosine receptor subtypes compared to related dihydropyridine analogs with smaller ester groups. PAF antagonist-1 can be used for cardiovascular disorders, especially hypertension and coronary heart disease .

HY-179605

AR ligand-49	Androgen Receptor	Others
AR ligand-49 (Compound 4q) is a dual ligand for the adenosine A_2A receptor (A_2AAR) and the A₃ receptor (A₃AR). Its K_i values are 15 and 4.5 nM respectively. AR ligand-49 exhibits reverse agonistic activity at hA_2AAR and antagonistic activity at hA₃AR. AR ligand-49 can be used for the study of the design and development of adenosine receptor ligands .

HY-180423

IRFI-165	Adenosine Receptor	Neurological Disease
IRFI-165 is a potent and selective A₁ adenosine receptor antagonist with a K_i of 7.9 nM for rat A₁ AR. IRFI-165 exhibies high selectivity versus A_2A and A₃ receptors. IRFI-165 induces antidepressant activity in vivo. IRFI-165 can be used for the research of psychiatric and neurological disorders .

HY-103166R

PSB-603 (Standard)	Reference Standards Adenosine Receptor	Inflammation/Immunology
PSB-603 (Standard) is the analytical standard of PSB-603 (HY-103166). This product is intended for research and analytical applications. PSB-603 is a potent and highly selective A2B adenosine receptor antagonist exhibiting a K_i value of 0.553 nM and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM .

HY-103190R

MRS1220 (Standard)	Reference Standards Adenosine Receptor	Neurological Disease Cancer
MRS1220 (Standard) is the analytical standard of MRS1220 (HY-103190). This product is intended for research and analytical applications. 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-153149

LJ-2698	Adenosine Receptor Apoptosis PGC-1α	Metabolic Disease Inflammation/Immunology
LJ-2698 is an orally active **adenosine A3 receptor** antagonist. LJ-2698 induces increased levels of anti-inflammatory cytokines in macrophages and significantly elevates the number of anti-inflammatory M2 macrophages in the lung. LJ-2698 prevents alveolar cavity enlargement, restores pulmonary function, inhibits matrix metalloproteinase activity and pulmonary cell apoptosis in the lung tissues of mice. LJ-2698 prevents renal injury, inhibits renal lipid accumulation, and increases PGC1α levels in renal tissues of mice with diabetic nephropathy. LJ-2698 is applicable to the research of emphysema and diabetic nephropathy .

Cat. No.	상품명	Category	Target	Chemical Structure

HY-119413

9-Ethyladenine	Natural Products Microorganisms Neurological Disease Classification of Application Fields Disease Research Fields Source Classification	Adenosine Receptor
9-Ethyladenine is a precursor of competitive antagonists of **adenosine receptors** (A₁, A₂, A₃), with no significant inhibitory effect on adenine phosphoribosyltransferase (APRT). 9-Ethyladenine derivatives have high affinity and selectivity for A₁ (K_i=27 nM), A₂A (K_i=46 nM), and A₃ (K_i=86 nM) receptors. 9-Ethyladenine does not inhibit brain APRT activity, can be used in the study of adenosine receptor-related diseases (such as nervous system diseases) models .

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adenosine A3 receptor antagonist

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