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A2A adenosine receptor agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenosine Receptor (38) Amyloid-β (1) Apoptosis (2) Drug Intermediate (3) Drug Metabolite (1) Endogenous Metabolite (7) Isotope-Labeled Compounds (4) Reference Standards (8)
By Research Areas:	Cancer (10) Cardiovascular Disease (14) Infection (1) Inflammation/Immunology (17) Metabolic Disease (1) Neurological Disease (14)
Oligonucleotides:	Adenosine (1) Nucleoside Analogs (1)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

Targets Recommended: Adenosine Kinase Adenosine Deaminase Adenosine Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N0092

Inosine 15+ Cited Publications	Adenosine Receptor Endogenous Metabolite	Neurological Disease Inflammation/Immunology Cancer
Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A₁ (A₁R) and A_2A (A_2AR) receptors .

HY-13201A

CGS 21680 Hydrochloride 10+ Cited Publications	Adenosine Receptor	Neurological Disease
CGS 21680 Hydrochloride is a selective **adenosine A2A receptor** agonist with a K_i of 27 nM.

HY-A0168

Regadenoson 3 Publications Verification CVT-3146	Adenosine Receptor	Cardiovascular Disease Cancer
Regadenoson (CVT-3146) is a selective **A2A adenosine receptor** agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .

HY-109139

Taminadenant 1 Publications Verification NIR178; PBF509	Adenosine Receptor	Neurological Disease Cancer
Taminadenant (NIR178; PBF509) is a highly potent and orally active **adenosine A_2A receptor** (A_2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with K_B values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response .

HY-12365

Namodenoson 3 Publications Verification CF-102; 2-Cl-IB-MECA	Adenosine Receptor	Cancer
Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (K_i=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively .

HY-103171

BAY 60-6583 5+ Cited Publications	Adenosine Receptor	Cardiovascular Disease Inflammation/Immunology
BAY 60-6583 is a potent and high-affinity agonist of adenosine A_2B receptor (EC₅₀=3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with K_i values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model .

HY-103181

N6-Cyclopentyladenosine CPA; UK-80882	Adenosine Receptor Apoptosis	Cardiovascular Disease Neurological Disease Cancer
N6-Cyclopentyladenosine (CPA) is a selective **Adenosine A₁ receptor** agonist, with K_i values of 2.3 nM, 790 nM and 43 nM for human A₁, A_2A and A₃ receptors, respectively. N6-cyclopentyladenosine increases Apoptosis. N6-Cyclopentyladenosine has antitumor activity against leukemia. N6-cyclopentyladenosine improves 5-fluorouracil (HY-90006)-induced hematopoietic damage, regulates sleep, and delays Aminophylline-induced clonic epileptic seizures .

HY-13201

CGS 21680 10+ Cited Publications	Adenosine Receptor	Neurological Disease
CGS 21680 is a selective **adenosine A2A receptor** agonist, with a K_i of 27 nM.

HY-N0092S2

Inosine-13C5 2 Publications Verification	Isotope-Labeled Compounds Adenosine Receptor Endogenous Metabolite	Neurological Disease Inflammation/Immunology Cancer
Inosine- ¹³C₅ is the ¹³C₅ labeled Inosine (HY-N0092). Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A₁ (A₁R) and A_2A (A_2AR) receptors .

HY-147400

Sipagladenant KW-6356	Adenosine Receptor	Neurological Disease
Sipagladenant (Compound I) is an orally active **adenosine receptor A2A** inverse agonist . Sipagladenant can be used in frontal lobe dysfunction research .

HY-103186

MRS-1706 1 Publications Verification	Adenosine Receptor	Inflammation/Immunology
MRS-1706 is a potent and selective **adenosine A_2B receptor** inverse agonist. MRS-1706 has K_i values of 1.39, 112, 157, and 230 nM for human A_2B, A_2A, A₁ and A₃ receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction .

HY-105068

Apadenoson BMS 068645; DWH 146e	Adenosine Receptor	Cardiovascular Disease
Apadenoson is an adenosine analog with selective agonist activity for the adenosine *A_2a* receptor and induces coronary vasodilatation .

HY-N0092R

Inosine (Standard)	Reference Standards Adenosine Receptor Endogenous Metabolite	Neurological Disease Inflammation/Immunology
Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A₁ (A₁R) and A_2A (A_2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A_2AR . Inosine dose-dependently induces hA_2AR-mediated ERK1/2 phosphorylation . Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes . In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .

HY-103183

CV1808 2-Phenylaminoadenosine	Adenosine Receptor Endogenous Metabolite	Inflammation/Immunology
CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with K_is of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively .

HY-Z9064

1-epi-Regadenoson ethyl ester	Drug Intermediate	Others
1-epi-Regadenoson ethyl ester is an intermediate in the synthesis of αisomer impurity of Regadenoson which is a highly selective adenosine A2A receptor agonist .

HY-103170

LUF5834	Adenosine Receptor	Others
LUF5834 is a selective A_2B adenosine receptor (A2BR) partial agonist (EC₅₀ = 12 nM). LUF5834 is also a partial *A₁/A_2A* adenosine receptor agonist (lacking selectivity) with K_i values of 2.6 and 28 nM, respectively .

HY-136233A

PSB 0777 ammonium hydrate	Adenosine Receptor	Inflammation/Immunology
PSB 0777 ammonium hydrate is a potent and selective adenosine *A_2A* receptor full agonist with K_i values of 44.4 nM, 360 nM for rat and human A_2A receptors, respectively. PSB 0777 ammonium hydrate has K_i values of ≥10000 nM, 541 nM for rat and human A₁ receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research .

HY-N0092S

Inosine-2,8-d2	Isotope-Labeled Compounds Adenosine Receptor Endogenous Metabolite	Neurological Disease Inflammation/Immunology
Inosine-2,8-d₂ is the deuterium labeled Inosine. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors .

HY-105017

Evodenoson ATL 313; DE 112	Adenosine Receptor	Infection Inflammation/Immunology
Evodenoson is a selective agonist of the **A_2A adenosine receptor*. Evodenoson’s primary actions include reducing inflammatory responses, decreasing intestinal fluid secretion, edema, tissue damage, and neutrophil infiltration induced by Clostridium difficile* toxin A. Evodenoson’s protective effect is achieved by reducing myeloperoxidase (MPO) and adenosine deaminase (ADA) activities, and by lowering the production of tumor necrosis factor-alpha (TNF-α) .

HY-106450

Binodenoson MRE-0470; WRC 0470	Adenosine Receptor	Cardiovascular Disease
Binodenoson (MRE-0470) is a potent and selective **A2A adenosine receptor** agonist (K_D=270 nM). Binodenoson is being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging .

HY-152656

2-Hydrazinyl-adenosine	Drug Intermediate Adenosine Receptor	Neurological Disease
2-Hydrazinyl-adenosine is a synthetic intermediate. Derivatives of 2-Hydrazinyl-adenosine act as *A_2A* adenosine receptor agonists. 2-Hydrazinyl-adenosine is used in the research of neurodegenerative diseases .

HY-120941

LASSBio-1359	Adenosine Receptor	Cardiovascular Disease Inflammation/Immunology
LASSBio-1359 is an **adenosine A2A receptor** agonist with vasodilatory and anti-inflammatory activities .

HY-Z9063

1-epi-Regadenoson	Drug Metabolite	Others
1-epi-Regadenoson is an αisomer impurity of Regadenoson which is a highly selective adenosine A2A receptor agonist .

HY-136233

PSB 0777 ammonium	Adenosine Receptor	Inflammation/Immunology
PSB 0777 ammonium is a potent and selective adenosine *A_2A* receptor full agonist with K_i values of 44.4 nM, 360 nM for rat and human A_2A receptors, respectively. PSB 0777 ammonium has K_i values of ≥10000 nM, 541 nM for rat and human A₁ receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research .

HY-N0092S1

Inosine-13C	Adenosine Receptor Isotope-Labeled Compounds Endogenous Metabolite	Neurological Disease Inflammation/Immunology Cancer
Inosine- ¹³C is the ¹³C labeled Inosine. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A₁ (A₁R) and A_2A (A_2AR) receptors .

HY-137370

2-Hexynyl-5′-N-ethylcarboxamidoadenosine HENECA; 2-Hexynyl-NECA	Adenosine Receptor Amyloid-β	Neurological Disease
2-Hexynyl-5′-N-ethylcarboxamidoadenosine (HENECA) is a selective **A_2A adenosine receptor** agonist. 2-Hexynyl-5′-N-ethylcarboxamidoadenosine increases intracellular cAMP level, and inhibits TNFα-evoked MMP-3 release. 2-Hexynyl-5′-N-ethylcarboxamidoadenosine induces Aβ42 production in SH-SY5Y cells .

HY-179681

A2A/A3 agonist-1	Adenosine Receptor	Inflammation/Immunology
A2A/A3 agonist-1 is a dual **A_2A/A₃ adenosine receptor** agonist. A2A/A3 agonist-1 has a K_i value of 2.9 nM and an EC₅₀ of 0.51 nM for hA_2AAR. A2A/A3 agonist-1 has a K_i of 0.8 nM and an EC₅₀ < 0.10 nM for hA₃AR. A2A/A3 agonist-1 possesses anti-inflammatory activity and can be used for the research of inflammatory diseases .

HY-A0168S

Regadenoson-d3 CVT-3146-d₃	Isotope-Labeled Compounds Adenosine Receptor	Cardiovascular Disease Cancer
Regadenoson-d₃ is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with K_is of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents .

HY-Z9065

1-epi-Regadenoson hydrazone	Drug Intermediate	Others
1-epi-Regadenoson hydrazone is an intermediate in the synthesis of αisomer impurity of Regadenoson which is a highly selective adenosine A2A receptor agonist .

HY-19310

AMP-579	Adenosine Receptor	Cardiovascular Disease Metabolic Disease
AMP-579 is an **adenosine receptor** agonist that primarily targets adenosine A1 and *A2_A* receptors (with K_i values of 1.7 and 4.5 nM for the A1 receptor in rat brain and adipocytes, and a K_i value of 56 nM for the *A2_A* receptor in rat brain). AMP-579 inhibits lipolysis, restores insulin-dependent glucose transport, and reduces heart rate through the activation of A1 receptors, while it induces vasodilation, particularly in coronary arteries, through the activation of *A2_A* receptors (with an IC₅₀ of 0.3 μM in porcine coronary arterial rings). AMP 579 shows potential for application in cardioprotection and the treatment of acute myocardial infarction .

HY-103183R

CV1808 (Standard) 2-Phenylaminoadenosine (Standard)	Reference Standards Adenosine Receptor Endogenous Metabolite	Inflammation/Immunology
CV1808 (Standard) is the analytical standard of CV1808. This product is intended for research and analytical applications. CV1808?(2-Phenylaminoadenosine) is a non-selective A2?adenosine receptor (A2 AR) agonist with Kis of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively .

HY-W777125

2-Chloro-3-deazaadenosine	Adenosine Receptor	Inflammation/Immunology
2-Chloro-3-deazaadenosine is agonists for **adenosine receptor, with K_i*s of 0.3, 0.08, 25.5 and 1.9 μM, for A1, A2A, A2B, and A3 receptors*, respectively .

HY-12365R

Namodenoson (Standard) CF-102 (Standard); 2-Cl-IB-MECA (Standard)	Reference Standards Adenosine Receptor	Cancer
Namodenoson (Standard) is the analytical standard of Namodenoson. This product is intended for research and analytical applications. Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (K_i=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively .

HY-A0168A

Regadenoson hydrate CVT-3146 hydrate	Adenosine Receptor	Cardiovascular Disease
Regadenoson hydrate (NSC 169186) is a selective **A2A adenosine receptor** agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson hydrate also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .

HY-103186R

MRS-1706 (Standard)	Reference Standards Adenosine Receptor	Inflammation/Immunology
MRS-1706 (Standard) is the analytical standard of MRS-1706. This product is intended for research and analytical applications. MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction .

HY-A0168R

Regadenoson (Standard) CVT-3146 (Standard)	Reference Standards Adenosine Receptor	Cardiovascular Disease
Regadenoson (Standard) is the analytical standard of Regadenoson. This product is intended for research and analytical applications. Regadenoson (CVT-3146) is a selective **A2A adenosine receptor** agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .

HY-103171R

BAY 60-6583 (Standard)	Reference Standards Adenosine Receptor	Cardiovascular Disease Inflammation/Immunology
BAY 60-6583 (Standard) is the analytical standard of BAY 60-6583. This product is intended for research and analytical applications. BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50?= 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model .

HY-W069173

2-Thioadenosine	Adenosine Receptor	Others
2-Thioadenosine is a selective A₁ adenosine receptor (A₁AR) ligand with a K_i of 80.3 nM. 2-Thioadenosine shows very low affinity for the A2A, A2B and A3 adenosine receptor subtypes. 2-Thioadenosine acts as a precursor for the synthesis of fluorescent A₃ adenosine receptor-selective agonists .

HY-108942

ASP5854	Adenosine Receptor	Cardiovascular Disease Neurological Disease
ASP5854 is an orally active, blood-brain barrier permeable adenosine *A1/A2a* dual receptor antagonist. ASP5854 blocks receptor activity and agonist-induced intracellular calcium elevation, and exhibits the characteristic of slow dissociation from striatal *A2a* receptors in primates. ASP5854 reverses catalepsy, enhances cognitive ability, improves motor function and exerts neuroprotective effects, while also alleviating dyskinesia and increasing contralateral turning behavior. ASP5854 is mainly used in studies related to ischemic stroke and Parkinson's disease .

HY-106450R

Binodenoson (Standard) MRE-0470 (Standard); WRC 0470 (Standard)	Reference Standards Adenosine Receptor	Cardiovascular Disease
Binodenoson (Standard) is the analytical standard of Binodenoson (HY-106450). This product is intended for research and analytical applications. Binodenoson (MRE-0470) is a potent and selective A2A adenosine receptor agonist (KD=270 nM). Binodenoson is being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging .

HY-103181R

N6-Cyclopentyladenosine (Standard) CPA (Standard); UK-80882 (Standard)	Reference Standards Adenosine Receptor Apoptosis	Cardiovascular Disease Neurological Disease Cancer
N6-Cyclopentyladenosine (Standard) is the analytical standard of N6-Cyclopentyladenosine (HY-103181). This product is intended for research and analytical applications. N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with K_i values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively. N6-cyclopentyladenosine increases Apoptosis. N6-Cyclopentyladenosine has antitumor activity against leukemia. N6-cyclopentyladenosine improves 5-fluorouracil (HY-90006)-induced hematopoietic damage, regulates sleep, and delays Aminophylline-induced clonic epileptic seizures .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0092

Inosine 15+ Cited Publications	Natural Products Human Gut Microbiota Metabolites Microorganisms Endogenous metabolite Source Classification	Adenosine Receptor Endogenous Metabolite
Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A₁ (A₁R) and A_2A (A_2AR) receptors .

HY-N0092R

Inosine (Standard)	Structural Classification Natural Products Human Gut Microbiota Metabolites Microorganisms Endogenous metabolite Source Classification	Reference Standards Adenosine Receptor Endogenous Metabolite
Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A₁ (A₁R) and A_2A (A_2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A_2AR . Inosine dose-dependently induces hA_2AR-mediated ERK1/2 phosphorylation . Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes . In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .

HY-103183

CV1808 2-Phenylaminoadenosine	Natural Products Classification of Application Fields Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Adenosine Receptor Endogenous Metabolite
CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with K_is of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively .

HY-103183R

CV1808 (Standard) 2-Phenylaminoadenosine (Standard)	Structural Classification Natural Products Endogenous metabolite Source Classification	Reference Standards Adenosine Receptor Endogenous Metabolite
CV1808 (Standard) is the analytical standard of CV1808. This product is intended for research and analytical applications. CV1808?(2-Phenylaminoadenosine) is a non-selective A2?adenosine receptor (A2 AR) agonist with Kis of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively .

Cat. No.	Product Name	Chemical Structure

HY-N0092S2

Inosine-13C5 2 Publications Verification
Inosine- ¹³C₅ is the ¹³C₅ labeled Inosine (HY-N0092). Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A₁ (A₁R) and A_2A (A_2AR) receptors .

HY-N0092S

Inosine-2,8-d2
Inosine-2,8-d₂ is the deuterium labeled Inosine. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors .

HY-N0092S1

Inosine-13C
Inosine- ¹³C is the ¹³C labeled Inosine. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A₁ (A₁R) and A_2A (A_2AR) receptors .

HY-A0168S

Regadenoson-d3

Regadenoson-d₃ is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with K_is of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents .

Cat. No.	Product Name		Classification

HY-152656

2-Hydrazinyl-adenosine		Nucleoside Analogs Adenosine
2-Hydrazinyl-adenosine is a synthetic intermediate. Derivatives of 2-Hydrazinyl-adenosine act as *A_2A* adenosine receptor agonists. 2-Hydrazinyl-adenosine is used in the research of neurodegenerative diseases .

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A2A adenosine receptor agonist

Inhibitors & Agonists

NaturalProducts

Isotope-Labeled Compounds

Oligonucleotides

Natural
Products