Home > Inhibitors & Agonists > GPCR > Adenosine Receptor
Cat. No. Product name CAS No.
DC8667 AB-MECA Featured

AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.

152918-26-8
DC10739 AZD4635 Featured

AZD4635 is a novel adenosine 2A receptor (A2AR) inhibitor with a Ki of 1.7 nM.

1321514-06-0
DC10440 Namodenoson (CF-102) Featured

CF-102(2-Cl-IB-MECA) is a selective A3 adenosine receptor agonist (Ki = 0.33 nM). Displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively. target: A3 adenosine receptor agonist;

163042-96-4
DC8471 CGS 21680 hydrochloride Featured

CGS 21680 hydrochloride is an A2A adenosine receptor agonist (Ki = 27 nM).

124431-80-7
DC10527 Ciforadenant (CPI-444) Featured

CPI-444 is an orally administered antagonist of the adenosine A2A receptor. It is designed to block the action of adenosine that is produced by tumors.

1202402-40-1
DCAPI1080 Istradefylline (KW-6002) Featured

Istradefylline(KW6002) is a very potent, selective and orally active adenosine A2A receptor antagonist(Ki=2.2 nM) in experimental models of Parkinson's disease.

155270-99-8
DC12258 MRS1186

MRS1186 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 7.66 nM.

183721-03-1
DC9805 Preladenant(SCH420814) Featured

Preladenant(SCH 420814) is a potent and selective antagonist at the adenosine A2A receptor.

377727-87-2
DC9332 Tozadenant

Tozadenant (SYN-115) is an adenosine A2A receptor antagonist.

870070-55-6
DC10946 TP455

TP455 (TP-455) is a highly potent, selective A2A adenosine receptor inverse agonist with IC50 of 1.9 nM in cyclic AMP assays in hA2A CHO cells.

2042563-95-9
DC8814 Vipadenant Featured

Vipadenant(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).

442908-10-3
DC7780 ZM241385 Featured

ZM 241385 is a Potent A2 adenosine receptor antagonist, with approx 50-fold selectivity for A2A receptors.

139180-30-6
DC11140 MSX-3 hydrate

261717-23-1
DC9284 SCH58261 Featured

SCH 58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively. Cas: 160098-96-4

160098-96-4
DC28031 AB928 Featured

AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist with immunomodulatory activity.

2239273-34-6
DC28421 MRS 1523

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.

212329-37-8
DC40019 DPCPX

DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes.

102146-07-6
DC40130 Xanthine amine congener dihydrochloride

Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2?receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model.

1962928-23-9
DC40225 FSCPX

FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modifies the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium.

156547-56-7
DC40855 PSB 0777 ammonium

PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki 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.

2122196-16-9
DC42123 Nitrobenzylthioinosine Featured

Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier.

38048-32-7
DC42304 SCH442416

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.

316173-57-6
DC42557 CD73-IN-4

CD73-IN-4 is a potent and selective methylenephosphonic acid CD73 inhibitor, with an IC50 of 2.6 nM for human CD73. CD73-IN-4 is potential for the research of cancer immunology.

2216764-29-1
DC44141 Trabodenoson

Trabodenoson (INO-8875), an adenosine mimetic, is a highly selective Adenosine A1 receptor agonist. Trabodenoson (INO-8875) is used in the study for Primary Open-Angle Glaucoma.

871108-05-3
DC45384 LUF6096

LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury.

1116652-18-6
DC45528 5'-N-Ethylcarboxamidoadenosine (NECA)

5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway.

35920-39-9
DC45783 Norisoboldine hydrochloride

Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.

5083-84-1
DC46391 PSB-10 hydrochloride

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.

591771-91-4
DC47006 A2B receptor antagonist 2

A2B receptor antagonist 2 (compound 18) is an adenosine receptor A2B antagonist, with Ki values of 2.30 μM, 6.8 μM and 3.44 μM for rA1, rA2A and hA2B, respectively.

784-90-7
DC47196 UK-432097

UK-432097 is a highly potent and selective A2AAR agonist with a pKi of 8.4 for human A2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research.

380221-63-6
DC47235 Binodenoson

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.

144348-08-3
DC47765 hA3AR agonist 1

hA3AR agonist 1 is a potent human A3 adenosine receptor (hA3AR) agonist with a Ki value of 2.40 nM.

DC47766 Adenosine receptor antagonist 1

Adenosine receptor antagonist 1 is a A2aR-selective antagonist with an IC50 of 0.29 nM and displays 14-fold more selective for A2aRthan A2bR.

2682930-40-9
DC47767 N6-Benzyl-5'-ethylcarboxamido adenosine

N6-Benzyl-5'-ethylcarboxamido adenosine is a selective A3 adenosine receptor agonist.

152918-32-6
DC49366 Heterobivalent ligand-1

Heterobivalent ligand-1 (compound 26) is a heterobivalent ligand for the Adenosine A 2A-dopamine D 2 receptor heteromer (KDB1 A2AR=2.1 nM, KDB1 D2R= 0.13 nM).

DC49612 A1AR antagonist 2

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.

1441961-74-5
DC49613 MRS1334

MRS1334 is a potent and selective human adenosine A3 receptor antagonist with Kis of 2.69 nM, >100 nM, >100 nM for hA3, rA1, rA2A, respectively. MRS1334 blocks the protective effect of Cl-IB-MECA leading to significant bradycardia and elevated ST segment.

192053-05-7
DC49614 Adenosine receptor antagonist 3

Adenosine receptor antagonist 3 is a potent antagonist of adenosine receptor. Adenosine receptor antagonist 3 has the potential for the research of cancer disease (extracted from patent WO2019233994A1, compound 1).

2400864-80-2
DC49615 IHCH-3064

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.

2420562-65-6
DC49616 A2A/A1 AR antagonist-1

A2A/A1 AR antagonist-1 (compound 1a) is dual potent A2A/A1 AR antagonist with Kis of 5.58 and 24.2 nM, respectively. A2A/A1 AR antagonist-1 has the potential for the research of ischemic stroke.

2445615-24-5
DC49617 Adenosine receptor antagonist 2

Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC50s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity.

2703054-47-9
DC49618 VUF-5574

VUF-5574 is a selective antagonist of adenosine A3 receptor with a Ki of 4.03 nM for the recombinant human receptor.

280570-45-8
DC49619 PSB36

PSB36 is a potent and selective antagonist of adenosine A1 receptor, with Kis 0.12 nM, 187 nM, 552 nM, 2300 nM, and 6500 nM for rA1, hA2B, rA2A, hA3 and rA3 receptors respectively. PSB36 can be used for the research of hyperalgesia.

524944-72-7
DC49620 A1AR antagonist 1

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.

DC70511 Inupadenant

Inupadenant (EOS-850, EOS100850) is a non brain-penetrant, potent and highly selective small molecule antagonist of adenosine A2a receptor (A2AR), shows activity at the high adenosine concentrations found in tumors.

2246607-08-7
DC71006 ATL-801

ATL-801, an A2B receptor selective antagonist, ameliorates murine colitis.

1000005-71-9
DC71212 hA2A/hCA XII modulator 1

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.

2548963-55-7
DC71216 (E)-8-(3-Chlorostyryl)caffeine

(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.

147700-11-6
DC71219 ANR94 Featured

ANR-94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR 94 has the potential for the research of Parkinson's disease.

634924-89-3
DC71325 Xanthine amine congener hydrochloride

Xanthine amine congener (XAC) hydrochloride is a non-selective adenosine receptor antagonist. Xanthine amine congener hydrochloride induces convulsions in mice.

1783977-95-6
DC71752 2'-MeCCPA Featured

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).

205171-12-6
DC71753 LJ-4517

LJ-4517 is a potent A2AAR antagonist, with a Ki of 18.3 nM. LJ-4517 is potent in displacing the binding of [3H]ZM241385 at WT A2AAR.

DC71754 PSB-0788

PSB-0788 (compound 17), xanthine-8-yl-benzenesulfonamide derivative, is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 (compound 17) can be used for the research for chronic inflammatory lung diseases.

1027513-54-7
DC71755 Sipagladenant Featured

Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist. Sipagladenant can be used in frontal lobe dysfunction research.

858979-50-7
DC71756 Theophylline sodium glycinate

Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline sodium glycinate inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline sodium glycinate induces apoptosis. Theophylline sodium glycinate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.

8000-10-0
DC71757 VCP171

VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain.

1018830-99-3
DC72032 M1069

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.

DC72243 L-Adenosine

L-Adenosine is a metabolically stable enantiomeric analog and also is a potential probe. L-Adenosine has weakly inhibitory adenosine deaminase (ADA) activity with an Ki value of 385 μM. L-Adenosine can be used for the research of adenosine uptake and accumulation.

3080-29-3
DC72615 PSB11 hydrochloride

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

453591-58-7
DC73370 BnOCPA

BnOCPA is a potent and powerful analgesic and a highly selective and potent, full agonist at human adenosine A1 receptors (A1Rs) with pEC50 of 7.23 in a NanoBRET agonist binding assay.

872693-38-4
DC73371 I-ABOPX

I-ABOPX (BW-A522) is a potent, selective A3 adenosine receptor antagonist with high affinity for both the ovine (Ki=3 nM) and human (Ki=19 nM) A3 receptors.

112533-64-9
DC73372 KF-26777

KF-26777 (KF26777) is a potent and selective adenosine A3 receptor antagonist with Ki of 0.2 nM (human A3 receptor).

206129-88-6
DC73373 MRS7935

MRS7935 is a potent, selective positive allosteric modulator (PAM) of A1 adenosine receptor (A1AR) with EC50 of 1.43 uM.

DC73374 OT-7999

OT-7999 (OT7999) is a potent and selective adenosine A3 receptor antagonist with Ki of 0.61 nM (human A3 receptor) in radioligand binding assays.

246031-23-2
DC73375 QAF-805 Featured

QAF-805 (QAF805) is a potent, dual adenosine-A2B receptor and adenosine-A3 receptor antagonist with Ki of 3.4 nM (A2B).

431040-19-6
DC73376 TRR469

TRR469 is a potent, selective adenosine A1 receptor (A1AR) positive allosteric modulator with pKb of 5.36, exhibits anti-nociceptive properties in acute and neuropathic pain models in mice.

1394867-58-3
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