Search Result
Results for "
adenosine receptors (AR)
" in MedChemExpress (MCE) Product Catalog:
8
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-147907
-
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Adenosine Receptor
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Neurological Disease
Inflammation/Immunology
Cancer
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Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases .
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- HY-101854
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N6-Phenethyladenosine; N6-Phenylethyladenosine
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Adenosine Receptor
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Inflammation/Immunology
Cancer
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N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine), an adenosine derivative, is a potent adenosine receptors (AR) agonist with Ki values of 11.8 nM, 30.1 nM, 0.63 nM for rat A1AR, human A1AR and hA3AR, respectively .
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- HY-111809
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Adenosine Receptor
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Others
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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 .
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- HY-101980
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HTL1071; AZD4635
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Adenosine Receptor
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Cancer
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AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors .
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- HY-120652
-
|
Adenosine Receptor
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Inflammation/Immunology
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A3AR antagonist 3 (compound 21) is a selective A3 adenosine receptor (A3AR) antagonist with a Ki of 37 nM. A3AR antagonist 3 shows >60-fold selectivity in comparison to A1 and A2A adenosine receptors .
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- HY-162851
-
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Adenosine Receptor
|
Others
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Adenosine receptor agonist 1 (compound 6m) is an A3 adenosine receptor (AR) partial agonist with Ki value of 6.7 nM .
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- HY-147908
-
|
Adenosine Receptor
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Inflammation/Immunology
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Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR .
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- HY-151899
-
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Adenosine Receptor
|
Inflammation/Immunology
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A3AR modulator 1 (MRS8054) is an orally active A3 adenosine receptor (A3AR) (Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [ 35S]GTPγS binding Emax .
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- HY-136702
-
|
Adenosine Receptor
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Inflammation/Immunology
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L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation .
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- HY-139694
-
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Adenosine Receptor
|
Others
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hA3AR agonist 1 is a potent human A3 adenosine receptor (hA3AR) agonist with a Ki value of 2.40 nM.
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- HY-103183
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-
-
- HY-124259
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-
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- HY-146457
-
|
Adenosine Receptor
|
Inflammation/Immunology
|
A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations .
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- HY-120090
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-
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- HY-N0138
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-
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- HY-118678
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-
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- HY-116042
-
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Adenosine Receptor
|
Cardiovascular Disease
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FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium .
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- HY-153333
-
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Adenosine Receptor
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Cardiovascular Disease
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A1/A3 AR antagonist 3 is an A1R/A3R dual antagonist with high affinity at low-micromolar to low-nanomolar. A1/A3 AR antagonist 3 can be used for the research of chronic heart diseases .
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- HY-147544
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-
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- HY-147543
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-
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- HY-147545
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-
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- HY-125602
-
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Adenosine Receptor
|
Neurological Disease
|
MNI-444 is a BBB-penetrable ligand of adenosine 2A receptor (A2AR). A2AR is a potential non-dopaminergic target for the research of Parkinson’s disease .
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- HY-103162
-
|
Adenosine Receptor
|
Neurological Disease
|
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 .
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- HY-161718
-
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Adenosine Receptor
|
Inflammation/Immunology
|
MRS8028 is an agonist for A3 adenosine receptor (A3AR), which binds hA3AR with Ki of 2.44 nM. MRS8028 is potential for ameliorating ischemia and inflammatory diseases .
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- HY-158180
-
|
Adenosine Receptor
|
Inflammation/Immunology
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A3AR agonist 4 is an A3 adenosine receptor (A3AR) agonist (Ki: 1.24 nM for hA3AR). A3AR agonist 4 inhibits cAMP production with an EC50 of 0.17 nM. A3AR agonist 4 can be used for research of inflammation and pain .
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- HY-147541
-
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Adenosine Receptor
|
Inflammation/Immunology
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A2A/A3 AR antagonist-1 (compound 23) is a dual A2A/A3 adenosine receptor (AR) fluorescent ligand, with Kis of 90 nM and 31.8 nM for hA2A AR and hA3 AR, respectively .
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- HY-167905
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-
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- HY-141865
-
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Adenosine Receptor
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Cancer
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Adenosine receptor antagonist 1 is a A2aR-selective antagonist with an IC50 of 0.29 nM and displays 14-fold more selective for A2aR than A2bR.
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- HY-144672
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-
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- HY-12099
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-
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- HY-158179
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Adenosine Receptor
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Neurological Disease
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A3AR agonist 3 (Compound 15A) is a A3 adenosine receptor (A3AR) agonist, with Ki and EC50 values of 2.27 and 0.20 nM for hA3 and cAMP, respectivelly. A3AR agonist 3 can be used for the research of neuroinflammation .
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- HY-158181
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Adenosine Receptor
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Inflammation/Immunology
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A3AR agonist 5 (Compound 6b) is a A3 adenosine receptor (A3AR) activator, with EC50 and Ki values of 0.14 nM and 6.36 nM for cAMP and hA3, respectively. A3AR agonist 5 can be used in pain and inflammatory research .
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- HY-161810
-
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Adenosine Receptor
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Others
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MRS8247 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR) that can also slow the dissociation rate of agonists .
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- HY-19532
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-
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- HY-164621
-
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Adenosine Receptor
|
Others
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A3AR antagonist 5 (Compound 16) is a selective antagonist for human adenosine A3 receptor with an affinity pC of 4.542 μM .
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- HY-144116
-
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Adenosine Receptor
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Neurological Disease
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A1AR antagonist 2 (compound 18h) is a potent A1 adenosine receptor (AR) antagonist with Kis of 1.49, 10.2, and 50.1 nM for hA1, hA2A and hA2B, respectively .
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- HY-144115
-
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Adenosine Receptor
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Neurological Disease
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A1AR antagonist 1 (compound 18g) is a potent A1 adenosine receptor (AR) antagonist with Kis of 2.08, 6.91, and 31.2 nM for hA1, hA2A and hA2B, respectively .
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- HY-101978
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CPI-444; V81444
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Adenosine Receptor
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Cancer
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Ciforadenant (CPI-444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses .
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- HY-110202
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- HY-N0092
-
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- HY-N0138S
-
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- HY-N0138S1
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-
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- HY-129393
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AB928
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Adenosine Receptor
|
Inflammation/Immunology
Cancer
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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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- HY-146456
-
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Adenosine Receptor
|
Neurological Disease
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A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases .
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- HY-N0138R
-
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Adenosine Receptor
Endogenous Metabolite
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Neurological Disease
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Theobromine (Standard) is the analytical standard of Theobromine. This product is intended for research and analytical applications. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
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- HY-103169
-
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Adenosine Receptor
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Neurological Disease
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SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain .
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- HY-W004425
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3,7-Dimethyl-1-propargylxanthine
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Adenosine Receptor
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Neurological Disease
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DMPX (3,7-Dimethyl-1-propargylxanthine) is a BBB-penatrable caffeine analogue. DMPX is A2 selective adenosine receptor (AR) antagonist that strongly and selectively blocks hypothermia and behavioral inhibition induced by A2 adenosine receptor agonists such as NECA (HY-103173). DMPX can be used in the study of Parkinson's disease and other diseases .
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- HY-N0092S1
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- HY-145308
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-
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- HY-12365
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CF-102; 2-Cl-IB-MECA
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Adenosine Receptor
|
Cancer
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Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively .
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- HY-106303
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Adenosine Receptor
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Cardiovascular Disease
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YT 146 is a potent agonist of A2 adenosine receptor (A2 AR) agonist. YT 146 causes a concentreation dependent cAMP accumulation, with the EC50 of 1.5 nM. YT 146 has cardioprotective effects .
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- HY-146478
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Adenosine Receptor
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Neurological Disease
Inflammation/Immunology
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A1/A3 AR antagonist 1 (compound 10) is a potent adenosine 1 (A1) and adenosine 3 (A3) receptor dual antagonist with Kis 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 .
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- HY-N0092S
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- HY-133862
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- HY-158882
-
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Biochemical Assay Reagents
Adenosine Receptor
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Others
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FLAC6 is a potent fluorinated detergent that can be used to solubilize membrane proteins (the native adenosine receptor A2AR, a G protein-coupled receptor, and two native transporters AcrB and BmrA). FLAC6 can maintain the structural and functional integrity of different membrane proteins .
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- HY-N0092S2
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- HY-109139A
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NIR178 mesylate; PBF509 mesylate
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Adenosine Receptor
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Cancer
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Taminadenant mesylate (NIR178 mesylate) is a potent adenosine A2A receptor antagonist with potential anti-tumor activity. Taminadenant mesylate can selectively bind and inhibit A2AR on T lymphocytes, thereby releasing adenosine/A2AR-mediated inhibition of T lymphocytes and activating T cell-mediated immune responses against tumor cells. Taminadenant mesylate works by reducing the proliferation of susceptible tumor cells. Taminadenant mesylate also showed effectiveness in reversing dyskinesias in Parkinson's disease models and was able to inhibit dyskinesias caused by L-DOPA .
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- HY-110012
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Adenosine Receptor
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Infection
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SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 μM .
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- HY-139644
-
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Adenosine Receptor
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Neurological Disease
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MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine .
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- HY-19532S
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- HY-103180
-
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Adenosine Receptor
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Neurological Disease
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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) .
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- HY-12365R
-
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Adenosine Receptor
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Cancer
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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 (Ki=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively .
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- HY-N0092S4
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- HY-103190
-
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Adenosine Receptor
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Neurological Disease
Cancer
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MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a Ki 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 .
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- HY-149916
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Adenosine Receptor
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Cancer
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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 (t1/2=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) .
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- HY-N0092S3
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- HY-N0092R
-
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Adenosine Receptor
Endogenous Metabolite
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Neurological Disease
Inflammation/Immunology
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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 A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR . Inosine dose-dependently induces hA2AR-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 .
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- HY-13591
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IB-MECA; CF-101
|
Adenosine Receptor
Apoptosis
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Inflammation/Immunology
Cancer
|
Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19 .
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- HY-P99483
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AT 004; VT 007
|
CD20
Adenosine Receptor
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Cancer
|
Blontuvetmab (AT 004) is a caninized CD20 monoclonal antibody and is also a potent, selective, highly potent antagonist of A2aR receptor. Blontuvetmab behaves as Nociceptin (HY-P0183)/Orphanin (HY-P0183) FQ receptor (NOP) agonists displaying weak NOP affinity. Blontuvetmab inhibits 5'-N-Ethylcarboxamidoadenosine (NECA)-mediated A2aR activation and significantly reverses the ability of adenosine to suppress CD8 T cell activation, increasing levels of cytokines such as IFN-γ. Blontuvetmab Blontuvetmab can be used for the research of Canine B-cell lymphoma .
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- HY-103177
-
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Adenosine Receptor
|
Inflammation/Immunology
|
PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice .
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- HY-109139
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NIR178; PBF509
|
Adenosine Receptor
|
Neurological Disease
Cancer
|
Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB 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 .
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- HY-145406
-
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Adenosine Receptor
HDAC
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Inflammation/Immunology
Cancer
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IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
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- HY-146979
-
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Adenosine Receptor
Carbonic Anhydrase
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Cancer
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hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research .
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- HY-115862
-
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Adenosine Receptor
PARP
Aurora Kinase
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Cardiovascular Disease
Cancer
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Benzo[c][1,8]naphthyridin-6(5H)-one exhibits low micromolar affinity to human adenosine receptor (AR) A1 and hA2A, with Ki of 4.6 and 4.8 μM. Benzo[c][1,8]naphthyridin-6(5H)-one is inhibitor for poly ADP-ribose polymerase-1 (PARP-1) and aurora kinase A, with IC50 of 0.311 and 5.5 μM .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99483
-
AT 004; VT 007
|
CD20
Adenosine Receptor
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Cancer
|
Blontuvetmab (AT 004) is a caninized CD20 monoclonal antibody and is also a potent, selective, highly potent antagonist of A2aR receptor. Blontuvetmab behaves as Nociceptin (HY-P0183)/Orphanin (HY-P0183) FQ receptor (NOP) agonists displaying weak NOP affinity. Blontuvetmab inhibits 5'-N-Ethylcarboxamidoadenosine (NECA)-mediated A2aR activation and significantly reverses the ability of adenosine to suppress CD8 T cell activation, increasing levels of cytokines such as IFN-γ. Blontuvetmab Blontuvetmab can be used for the research of Canine B-cell lymphoma .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-N0138S
-
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Theobromine-d6 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
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- HY-N0138S1
-
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Theobromine-d3 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
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- HY-N0092S
-
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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 .
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- HY-N0092S2
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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 A2A (A2AR) receptors .
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- HY-N0092S1
-
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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 A2A (A2AR) receptors .
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- HY-19532S
-
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ZM241385-d7 is a deuterated form of ZM241385 (HY-19532). 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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- HY-N0092S4
-
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Inosine-13C3 is a 13C-labeled Inosine that can be used in pharmacokinetic studies of Inosine. Inosine is an agonist of adenosine receptors A1R and A2AR with anti-inflammatory immunomodulatory, antinociceptive and neuroprotective effects .
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- HY-N0092S3
-
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Inosine-13C10,15N4 is 13C and 15N 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 A2A (A2AR) receptors .
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