1. Signaling Pathways
  2. GPCR/G Protein
  3. Adenosine Receptor

Adenosine Receptor

Receptor

P1 receptor

Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes have been cloned and identified in different tissues. These receptors have distinct localization, signal transduction pathways and different means of regulation upon exposure to agonists. A key property of some of Adenosine receptors is their ability to serve as sensors of cellular oxidative stress, which is transmitted by transcription factors, such as NF-κB, to regulate the expression of ARs. The importance of Adenosine receptors in the regulation of normal and pathological processes such as sleep, the development of cancers and in protection against hearing loss will be examined.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18776
    A2AR-agonist-1
    Agonist 99.90%
    A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.
    A2AR-agonist-1
  • HY-147400
    Sipagladenant
    Modulator 99.82%
    Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist. Sipagladenant can be used in frontal lobe dysfunction research.
    Sipagladenant
  • HY-111809
    N6-Ethyladenosine
    Agonist 99.90%
    N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively.
    N6-Ethyladenosine
  • HY-103164
    (E)-8-(3-Chlorostyryl)caffeine
    Antagonist 99.4%
    (E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research.
    (E)-8-(3-Chlorostyryl)caffeine
  • HY-148088
    M1069
    Antagonist 98.04%
    M1069 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 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.
    M1069
  • HY-B0809R
    Theophylline (Standard)
    Inhibitor 99.99%
    Theophylline (Standard) is the analytical standard of Theophylline. This product is intended for research and analytical applications. Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
    Theophylline (Standard)
  • HY-B1742
    Proxyphylline
    Antagonist 99.93%
    Proxyphylline is a methylxanthine derivative used as a cardiac stimulant, vasodilator and bronchodilator.
    Proxyphylline
  • HY-103180
    2-Chloro-N-cyclopentyl-2′-C-methyladenosine
    Agonist 99.80%
    2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs).
    2-Chloro-N-cyclopentyl-2′-C-methyladenosine
  • HY-111082
    ISAM-140
    Inhibitor 99.85%
    ISAM-140 (22b) is a potent and highly selective A2B adenosine receptor antagonist with a Ki of 3.49 nM.
    ISAM-140
  • HY-123085
    Alloxazine
    Antagonist
    Alloxazine is a selective A2b antagonist. Alloxazine completely block 5’N-Ethylcarboxamido adenosine (NECA)-mediated cyclic AMP accumulation with an IC50 of 2.9 μM. Alloxazine can be used for the research of cancer.
    Alloxazine
  • HY-106841
    Draflazine
    99.06%
    Draflazine (R-75231) is a ENT1 inhibitor. Draflazine (R-75231) completely reverses the hypersensitivity in the complete Freund’s adjuvant (CFA) model of mechanical hyperalgesia and the carrageenan inflammation model of thermal and mechanical hyperalgesia.
    Draflazine
  • HY-13236
    LUF6000
    Agonist 99.09%
    LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect.
    LUF6000
  • HY-106199
    Adenosine A1 receptor activator T62
    Activator 98.93%
    Adenosine A1 receptor activator T62 is an allosteric enhancer of adenosine A1 receptor. Adenosine A1 receptor activator T62 produces antinociception in animal models of acute pain and also reduces hypersensitivity in models of inflammatory and nerve-injury pain.
    Adenosine A1 receptor activator T62
  • HY-103162
    ANR94
    Antagonist
    ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease.
    ANR94
  • HY-101300
    Cirazoline hydrochloride
    Agonist 99.65%
    Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM).
    Cirazoline hydrochloride
  • HY-19365
    AB-MECA
    Agonist 98.32%
    AB-MECA is a high affinity A3 adenosine receptor agonist with a binding Ki of 430.5 nM for human A3 receptors in CHO cells. AB-MECA can enhance plasma histamine level.
    AB-MECA
  • HY-19842
    GS-9667
    Agonist 98.08%
    GS-9667 (CVT 3619), a novel N6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA).
    GS-9667
  • HY-116800
    FR194921
    Antagonist 98.10%
    FR194921 is a potent, selective and orally active and cross the blood-brain barrier Adenosine A1 antagonist with Ki value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity.
    FR194921
  • HY-W011955
    8-Cyclopentyl-1,3-dimethylxanthine
    Antagonist 99.82%
    8-Cyclopentyl-1,3-dimethylxanthine (Compound 2a) is a selective adenosine A1 receptor antagonist with Kis of 10.9 nM and 1440 nM for A1 receptor and A2 receptor, respectively.
    8-Cyclopentyl-1,3-dimethylxanthine
  • HY-A0181S
    Adenosine monophosphate-13C10,15N5 dilithium
    Agonist ≥99.0%
    Adenosine monophosphate-13C10,15N5(AMP-13C10,15N5) is the 13C-labeled and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction.
    Adenosine monophosphate-<sup>13</sup>C<sub>10</sub>,<sup>15</sup>N<sub>5</sub> dilithium
Cat. No. Product Name / Synonyms Application Reactivity

Adenosine A1 receptor (A1R)

Adenosine A2A receptor (A2AR)

Adenosine A2B receptor (A2BR)

Adenosine A3 receptor (A3R)

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Please try each isoform separately.

Adenosine Receptor Inhibitors, Agonists, Antagonists & Modulators
Product NameAdenosine A1 receptor (A1R)Adenosine A2A receptor (A2AR)Adenosine A2B receptor (A2BR)Adenosine A3 receptor (A3R)Purity    
Inosine
A1AR
A2AR
  99.67%
ZM241385 
A2AR, Ki: 1.4 nM
  99.45%
Adenosine 5'-monophosphate disodium  
A2BR
 99.63%
DPTN dihydrochloride   
hA3, Ki: 1.65 nM
98.66%
Derenofylline
A1R, Ki: 1 nM
A2AR, Ki: 398 nM
 
Adenosine A3 receptor, Ki: 200 nM
99.93%
PSB-1115  
A2BR
 ≥99.0%
MIPS521
A1AR
   98.21%
(E)-8-(3-Chlorostyryl)caffeine 
A2AR
  99.4%
M1069 
A2AR
A2BR
 98.04%
2-Chloro-N-cyclopentyl-2′-C-methyladenosine
A1AR
   99.80%
ISAM-140  
hA2B, Ki: 3.49 nM
 99.85%
ANR94 
A2AR, Ki: 46 nM (human)
  
AB-MECA   
Adenosine A3 receptor
98.32%
FR194921
A1R, Ki: 6.6 nM
A2AR, Ki: 5400 nM
  98.10%
Evodenoson 
A2AR
  99.74%
VUF-5574   
Recombinant Human Adenosine A3 receptor (A3R) , Ki: 4.03 nM
99.41%
Adenosine receptor antagonist 2 
A2a adenosine receptor, IC50: 1 nM
A2b adenosine receptor, IC50: 3 nM
  99.37%
PSB36
rA1, Ki: 0.12 nM
rA2A, Ki: 552 nM
hA2B, Ki: 187 nM
hA3, Ki: 2300 nM
rA3, Ki: 6500 nM
≥99.0%
Adenosine receptor inhibitor 1
A1AR, Ki: >1000 nM
A2AR, Ki: 68.5 nM
hA2B, Ki: >1000 nM
Adenosine A3 receptor, Ki: >1000 nM
98.29%
MRS1334
rA1, Ki: >100 nM
rA2A, Ki: >100 nM
 
hA3, Ki: 2.69 nM
≥99.0%
LUF5834
A1R, Ki: 2.6 nM
A2AR, Ki: 28 nM
A2BR, EC50: 12 nM
 99.8%
A2AAR antagonist 2 
A2a adenosine receptor, IC50: 33.5 nM
  
Adenosine receptor inhibitor 2
A1AR, Ki: 52.2 ± 8.5 nM
A2AR, Ki: 167 ± 22 nM
hA2B, Ki: >1000 nM
Adenosine A3 receptor, Ki: >1000 nM
A1AR antagonist 5
hA1AR, pKi: 6.11
hA2AAR, pKi: <4
  
GW-493838
A1AR
   
MRS3558 
hA2AAR, Ki: 0.6 nM
rA2A, Ki: 0.9 nM
  
ST 1535 
A2a adenosine receptor
  99.80%
A1AR antagonist 4
hA1AR, pKi: 6.29
hA2AAR, pKi: <4
  
PSB11 hydrochloride   
human A3, Ki: 2.3 nM
hA3AR agonist 1   
Adenosine A3 receptor, Ki: 2.40 nM
LAS38096
A1, Ki: >1000 nM
A2A, Ki: >2500 nM
A2B, Ki: 17 nM
A3, Ki: >1000 nM
Adenosine receptor antagonist 5   
human A3, Ki: 12 nM
LJ-4517 
A2AR, Ki: 18.3 nM
  
A3AR antagonist 3
hA1AR, Ki: 2.22 μM
hA2AAR, Ki: 7.73 μM
 
hA3, Ki: 37 nM
CP-608039   
Adenosine A3 receptor
SCH-202676   
Adenosine A3 receptor
A3AR agonist 4   
human A3, Ki: 1.24 nM
A3AR modulator 1   
Adenosine A3 receptor
A1AR antagonist 6
hA1AR, pKi: 7.13
hA2AAR, pKi: <4
  
ATL444
rA1, Ki: 7.0 nM
rA2A, Ki: 2.5 nM
A2BR, Ki: 61.8 nM
rA3, Ki: >1000 nM
A2A receptor antagonist 3
A1R, Ki: 107 nM
A2AR, Ki: 0.4 nM
A2BR, Ki: 37 nM
A3R, Ki: 1467 nM
hA2A/hCA XII modulator 1
hA1AR, Ki: 4.819 μM
hA2AAR, Ki: 6.4 nM
 
hA3, Ki: >30 μM
A2AR-antagonist-1 
A2AR, IC50: 29 nM
  
VCP171
A1R
   
A2AAR/HDAC-IN-1
A1AR, Ki: 503.3 ± 14 nM
A2AR, Ki: 163.5 ± 14 nM
hA2B, Ki: >10000 nM
Adenosine A3 receptor, Ki: >10000 nM
Neladenoson dalanate hydrochloride
A1R
   
A2A receptor antagonist 2 
A2AR, IC50: 8.3 nM
  
A3AR antagonist 1   
hA3, Ki: 4.63 nM
A3AR antagonist 2   
hA3, Ki: 4.54 nM
A2AR/A2BR antagonist 1 
A2AR, IC50: 11.2 nM
A2BR, IC50: 6.4 nM
 
Neladenoson dalanate
A1R
   
YT 146 
A2AR
  
MRS5698   
Adenosine A3 receptor, Ki: ~3 nM
A2A/A3 AR antagonist-1 
hA2AAR, Ki: 90 nM
 
hA3, Ki: 31.8 nM
A1AR antagonist 3
human A1, Ki: 9.69 nM
rat A1, Ki: 0.529 nM
   
A1/A3 AR antagonist 1
human A1, Ki: 36.7 nM
rat A1, Ki: 1.47 nM
  
human A3, Ki: 25.4 nM
Adenosine receptor antagonist 1 
A2AR, IC50: 0.29 nM
  
2-Chloro-3-deazaadenosine
A1, Ki: 0.3 μM
A2A, Ki: 0.08 μM
A2B, Ki: 25.5 μM
A3, Ki: 1.9 μM
MRE 0094 
A2A, Ki: 0.49 μM
A2B, Ki: 10 μM
 
Benzo[c][1,8]naphthyridin-6(5H)-one
hA1AR, Ki: 4.6 μM
hA2AAR, Ki: 4.8 μM
  
CVT-2759 analog
A1, Ki: 167 nM
   
CVT-5440
A1, Ki: >10 (Pan)
A2A, Ki: >5 (Pan)
A2B, Ki: 50 nM
 
MRS1067   
Adenosine A3 receptor
CGH2466 dihydrochloride
A1, IC50: 19 nM
 
A2B, IC50: 21 nM
A3, IC50: 80 nM
Adenosine receptor agonist 1   
hA3, Ki: 6.7 nM
VUF8504
human A1, Ki: 14 nM
  
human A3, Ki: 0.017 nM
GW 328267 
A2a adenosine receptor
  
FLAC6 
A2AR
  
2-Hexynyl-5′-N-ethylcarboxamidoadenosine 
A2AR